CFI-402257_DataSheet_MedChemExpress
BFH772_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC 50 value of 3 nM.IC50 & Target: IC50: 2.7±0.9 nM (hVEGFR2), 1.5±0.53 μM (mVEGFR2), 1.7±0.36 μM (hVEGFR1), 1.1±0.29 μM (hVEGFR3)[1]In Vitro: BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC 50, it also targets B–RAF, RET, and TIE–2, albeit with atleast 40–fold lower potency. BFH772 is inactive (IC 50>10 μM; >2 μM for cKIT) against all other tyrosine specific– andserine/threonine–specific protein kinases tested. BFH772 inhibits VEGFR2 with IC 50 of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC 50 of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases,with IC 50 values ranging between 30 and 160 nM. BFH772 is selective (IC 50 values >0.5 μM) against the kinases of EGFR, ERBB2,INS–R, and IGF–1R and against the cytoplasmic BCR–ABL kinase. IC 50 of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations [1].In Vivo: BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54–90% for primary tumor and71–96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene–1–carboxamide inhibits VEGF induced tissue weight and TIE–2 levels but only reaches statistical significance at 1 mg/kg and above [1].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]In vitro kinase assay is based on a filter binding assay, using the recombinant GST–fused kinase domainsexpressed in baculovirus and purified over glutathione–sepharose, γ–[33P]ATP as the phosphate donor, and poly(Glu:Tyr 4:1) peptide as the acceptor. Each GST–fused kinase is incubated under optimized buffer conditions [20 mM Tris–HCl buffer (pH 7.5), 1–3 mM MnCl 2, 3–10 mM MgCl 2, 3–8 μg/mL poly(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1mM DTT] and 0.2 μCi γ–33P ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 min at ambient temperature. The reaction is stopped by adding 10 mL of 250 mM EDTA. Using a 384–well filter system, half the volume istransferred onto an Immobilon–polyvinylidene difluoride membrane. The membrane is then washed extensively and dried, and scintillation counting is performed. IC 50s for compounds are calculated by linear regression analysis of the percentage inhibition [1].Cell Assay: BFH772 is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate medium before use [1]. [1]DifferentBa/F3 cell lines rendered IL–3 independent by transduction with various constitutively active tyrosine kinases are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental Ba/F3 cells, the medium is additionally supplemented with 10 ng/mL interleukin–3 (IL–3). For proliferation assays, Ba/F3 cells are seeded on 96–well plates in triplicates at 10000 cells per well and incubated with various concentrations of compounds for 72 h followed by quantification of viable cells using a resazurin sodium salt dye reduction readout (commercially known as Alamar Blue assay). IC 50s are determined with the XLFit Excel Add–In using a four–parameter dose response model [1].Animal Administration: BFH772 is prepared in PEG200 100% (Mice)[1].Product Name:BFH772Cat. No.:HY-100419CAS No.:890128-81-1Molecular Formula:C 23H 16F 3N 3O 3Molecular Weight:439.39Target:VEGFR Pathway:Protein Tyrosine Kinase/RTK Solubility:DMSO: 7.75 mg/mLBFH772 is dissolved in N–methyl pyrrolidone/polyethylene glycol200 (30:70, v/v) (Rat)[1].[1]Mice[1]Female FVB mice weighing between 18 and 20 g are housed in groups of six. Porous chambers containing VEGF (2 μg/mL) in 0.5 mL of 0.8% w/v agar (containing heparin, 20 U/mL) are implanted subcutaneously in the flank of the mice (n=6 per group). VEGF induces the growth of vascularized tissue around the chamber. This response is dose–dependent and can be quantified by measuring the weight and TIE–2 levels of the tissue. Mice are treated either orally once daily with compounds or vehicle (PEG200 100%, 5 mL/kg) starting4–6 h before implantation of the chambers and continuing for 4 days. The animals are sacrificed for measurement of the vascularized tissues 24 h after the last dose. Tissue weight is taken and then a lysate prepared for TIE–2 ELISA analysis .Rat[1]Catheters are implanted into the femoral artery and vein of na?ve female rats strain OFA for BFH772, and BAW2881, or in the jugular vein and femoral artery in female Sprague–Dawley rats for compounds 4, 9, and 10. Animals are allowed to recover for 96 h and are housed in single cages with free access to food and water throughout the experiment. Female OFA rats received 2.5 mg/kg ofBAW2881 dissolved in ethanol/dimethylisosorbide/polyethylene glycol400/D5W (10/15/35/40 v/v) or 1 mg/kg of BFH772 dissolved in N–methyl pyrrolidone/polyethylene glycol200 (30:70, v/v) via injection into the femoral vein. D5W is glucose 5%/water (v/v). Oral administration: BAW2881 and BFH772 are formulated as a micronized suspension (dissolved/suspended in 0.5% carboxymethyl cellulose in distilled water) and administered by gavage to female OFA rats to deliver a dose of 25 mg/kg for BAW2881 or 3 mg/kg BFH772 (n=4 rats per group). For compounds 4, 9, and 10, female Sprague–Dawley rats at 8 weeks of age received an intraveno References:[1]. Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132–46.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
HT-2157_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:HT–2157 (SNAP 37889) is a selective, high–affinity, competitive antagonists of galanin–3 receptor (Gal 3).IC50 & Target: Galanin–3 receptor [1]In Vitro: HT–2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK – cells expressing the human Gal 3 receptor (K i =17.44±0.01 nM; n>100) and is highly selective for Gal 3 over the Gal 1 and Gal 2 subtypes (K i >10,000 nM for each subtype; n=46 of each subtype). When tested for the antagonism of galanin–evoked inhibition of adenylyl cyclase, HT–2157 (0.1–10μM) produces concentration–dependent rightward shifts of the concentration–effect curve to galanin [1].In Vivo: The galanin–3 receptor antagonist, HT–2157 (SNAP 37889), reduces operant responding for ethanol in alcohol–preferring rats. The novel selective GALR3 antagonist, HT–2157, to reduce anxiety–like behaviour and voluntary ethanol consumption in the iP (alcohol–preferring) rat. Male iP rats treated with HT–2157 at a dose of 30 mg/kg (i.p.) do not show altered locomotor activity or changes in anxiety–like behaviour in the elevated plus maze or light–dark paradigms. Treatment with HT–2157 (30 mg/kg, i.p.)reduces operant responding for solutions containing ethanol, sucrose and saccharin. Collectively, results from the current study shows that HT–2157 (30 mg/kg, i.p.) is effective in reducing operant responding for ethanol, independent of a sedative effect [2].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]Binding affinities for HT–2157 (SNAP 37889) and SNAP 398299 at the human Gal 1, Gal 2, and Gal 3 receptors are determined by using the 125I–galanin displacement assay. Additionally, is tested for binding in a broad cross–reactivity panel that included G–protein–coupled receptors, ion channels, enzymes, and transporters. The ability of HT–2157 to antagonize functional responses to galanin is examined in modified HEK–293 cells (PEAK rapid cells) transiently cotransfected with the Gal 3 receptor and Gαz by measuring the inhibition of adenylyl cyclase activity [1].Animal Administration: HT–2157 (SNAP 37889) is prepared in 5% DMSO and 1% HMC in saline [2].[2]Rat [2]The effect of HT–2157 on locomotor activity is examined using adult male iP rats (n=12; 418–467 g). Locomotor activity is tested to ensure that any potential change in anxiety or ethanol consumption in subsequent tests is not due to any sedative property of the drug. Rats are habituated to the locomotor cells (26×26×40 cm) for 60 minute sessions which are conducted daily for threeconsecutive days. To minimise the effect of habituation during the treatment phase, rats are divided into two even groups which received a single injection of either HT–2157 (30 mg/kg, i.p.) or vehicle (1 ml/kg i.p.) 30 min prior to being placed in the locomotor cells for a 60 minute session. The following day the treatments are reversed so that all rats received treatment with both the vehicle and SNAP 37889 compound. Movements in terms of number of moves, move time (s) and total distance travelled (cm), are recorded automatically using TruScan 2.0 software.References:Product Name:HT–2157Cat. No.:HY-100717CAS No.:303149-14-6Molecular Formula:C 21H 13F 3N 2O Molecular Weight:366.34Target:Neuropeptide Y Receptor Pathway:GPCR/G Protein Solubility:DMSO: ≥ 29 mg/mL[1]. Swanson CJ, et al. Anxiolytic– and antidepressant–like profiles of the galanin–3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489–94.[2]. Ash BL, et al. The galanin–3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol–preferring rats. Regul Pept. 2011 Jan 17;166(1–3):59–67.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
宫腔镜子宫内膜息肉切除术治疗子宫内膜息肉患者的应用效果
临床医学China &Foreign Medical Treatment 中外医疗宫腔镜子宫内膜息肉切除术治疗子宫内膜息肉患者的应用效果蒙霞，韦淑向河池市第一人民医院妇科，广西河池 546300［摘要］ 目的 探究宫腔镜子宫内膜息肉切除术治疗子宫内膜息肉患者的效果。
方法 方便选取2021年6月—2023年6月河池市第一人民医院收治的86例子宫内膜息肉患者为研究对象，按照随机数表法分为两组，各43例。
对照组予以宫腔镜下刮宫术，观察组予以宫腔镜子宫内膜息肉切除术，对比两组治疗疗效、月经情况及子宫内膜、性激素水平与术后并发症发生情况。
结果 观察组治疗有效率（97.67%）高于对照组（83.72%），差异有统计学意义（χ2=4.962，P <0.05）。
治疗6个月后，观察组月经期、月经量、子宫内膜厚度分别为（5.42±1.08）d 、（56.48±10.26）分、（3.94±0.98）mm ，均优于对照组，差异有统计学意义（t =5.998、6.604、3.825，P 均<0.05）。
观察组黄体生成素、孕酮分别为（4.19±0.54）IU/L 、（1.18±0.11）pg/mL 均高于对照组，雌二醇（62.26±11.26）pg/mL 低于对照组，差异有统计学意义（t =8.564、6.848、5.847，P 均<0.05）。
观察组并发症发生率（2.33%）低于对照组（13.95%），差异有统计学意义（χ2=3.888，P <0.05）。
结论 宫腔镜子宫内膜息肉切除术用于子宫内膜息肉治疗上具有显著成效，能进一步改善患者术后月经情况及子宫内膜厚度，且维持患者机体性激素水平，降低治疗后并发症发生率。
［关键词］ 宫腔镜；子宫内膜息肉切除术；月经量；子宫内膜厚度；并发症［中图分类号］ R5 ［文献标识码］ A ［文章编号］ 1674-0742（2024）02(c)-0053-05Effect of Hysteroscopic Endometrial Polyp Resection on Patients with En⁃dometrial PolypsMENG Xia, WEI ShuxiangDepartment of Gynecology, Hechi First People's Hospital, Hechi, Guangxi Zhuang Autonomous Region, 546300 China [Abstract] Objective To explore the effect of hysteroscopic resection of endometrial polyps in the treatment of patients with endometrial polyps. Methods A total of 86 patients with endometrial polyps from the First People's Hospital of He⁃chi City from June 2021 to June 2023 were conveniently selected as the study objects and divided into two groups ac⁃cording to random number table method, with 43 patients in each group. The control group was given hysteroscopic cu⁃rettage, and the observation group was given hysteroscopic resection of endometrial polyps. The therapeutic efficacy, menstrual status, endometrial, sex hormone levels and postoperative complications were compared between the two groups. Results The effective rate of the observation group (97.67%) was higher than that of the control group (83.72%), and the difference was statistically significant (χ2=4.962, P <0.05). After 6 months of treatment, the menstrual period, menstrual volume and endometrial thickness in the observation group were (5.42±1.08) d, (56.48±10.26) min and (3.94±0.98) mm, respectively, which were better than those in the control group, and the differences were statistically significant (t =5.998, 6.604, 3.825, all P <0.05). Luteinizing hormone (4.19±0.54) IU/L and progesterone (1.18±0.11) pg/mL in the observation group were higher than those in the control group, and estradiol (62.26±11.26) pg/mL were lowerthan those in the control group, and the differences were statistically significant (t =8.564, 6.848, 5.847, all P <0.05). The complication rate of observation group (2.33%) was lower than that of control group (13.95%), and the difference was statistically significant (χ2=3.888, P <0.05). Conclusion Hysteroscopic resection of endometrial polyps has signifi⁃DOI ：10.16662/ki.1674-0742.2024.06.053[作者简介] 蒙霞（1979-），女，壮族，本科，副主任医师，研究方向为子宫内膜息肉切除术。
解说清喉消炎颗粒的薄层色谱鉴别
解说清喉消炎颗粒的薄层色谱鉴别【摘要】目的建立清喉消炎颗粒的薄层色谱鉴别方法。
方法采用薄层色谱法对清喉消炎颗粒中的板蓝根、地胆草、甘草等药材进行了鉴别。
结果薄层色谱法能清晰地鉴别清喉消炎颗粒中的板蓝根、地胆草、甘草，阴性无干扰。
结论建立的薄层色谱法操作简单，斑点清晰,分离度好，重现性好，可作为清喉消炎颗粒的质量控制方法。
【关键词】清喉消炎颗粒;薄层色谱;板蓝根;地胆草;甘草清喉消炎颗粒是由板蓝根、地胆草、甘草等中药组成。
该制剂是按医院协定的处方改革而得到的新剂型，具有清热解毒、凉血利咽的功效。
可用于咽喉肿痛等症状。
本文对清喉消炎颗粒处方中的板蓝根、地胆草、甘草等中药进行了薄层鉴别，从而为其质量控制提供必要的依据。
1、仪器与试药1.1 仪器ZF90型暗箱式紫外透射仪(上海顾村电光仪器厂)，定量点样毛细管,国产薄层预制G板(青岛海洋化工厂分厂)，国产薄层预制GF254板(青岛海洋化工厂分厂)。
1.2 试药板蓝根药材、甘草药材、地胆草药材均由广东药学院药用植物学教研室李书渊教授鉴定;靛玉红对照品(中国药品生物制品检定所， 7179402);甘草次酸对照品(中国药品生物制品检定所，723200109);清喉消炎颗粒(规格为10 g/袋，批号为20060601，20060602，200606030)、板蓝根阴性对照样品、地胆草阴性对照样品、甘草阴性对照样品均由广州医学院第二附属医院提供，其余试剂均为分析纯。
2、实验部分2.1 板蓝根的薄层鉴别取本品颗粒50 g，加入硫酸钠饱和的水溶液80 mL 溶解，转移至分液漏斗中，用乙醚振摇提取3次，每次30 mL，合并乙醚液，用质量分数为1%的氢氧化钠溶液洗涤3次，每次30 mL，再用水洗涤3次，每次30 mL，取乙醚液，水浴上蒸干，残渣加二氯甲烷约0.5 mL使其溶解，作为供试品溶液。
另取板蓝根对照药材6 g，加无水乙醇适量，加热回流1 h，滤过，滤液于水浴上蒸干，残渣加入硫酸钠饱和的水溶液20 mL溶解，同法制成对照药材溶液。
北京春达科技有限公司专营进口体外诊断试剂工业原料，透析产品，纯化填料，标准品
北京春达科技有限公司专营进⼝体外诊断试剂⼯业原料，透析产品，纯化填料，标准品SCLPP209碱性磷酸酶3.1.3.1Alkaline phosphatase from Calf intestine-Activity: >30000 U/mlGlycerol solution-Mw: 100,000-Store at -20 °CSCMAD211苹果酸脱氢酶1.1.1.37Malate dehydrogenase from Microorganism-Activity: >40 U/mgYellowish amorphous powder-Mw: 140,000-Store at -20 °CSCMDH18C苹果酸脱氢酶1.1.1.37Malate dehydrogenase from Pig heart-Activity: >1250 U/mgprot.White amorphous powder-Mw:140,000-Store at -20 °CSCMDL100苹果酸脱氢酶1.1.1.37Malate dehydrogenase from Microorganism-Activity: >60 U/mgWhite amorphous powder-Mw: 80,000-Store at -20 °CSCMUT11C变旋酶5.1.3.3Mutarotase from Porcine kidney-Activity: >1500 U/mgWhite amorphous powder-Mw: 40,000-Store at -20 °CSCMUT12C变旋酶5.1.3.3Mutarotase from Porcine kidney-Activity: >1000 U/mlAmmonium sulfate suspension-Mw: 40,000-Store at 2-8 °CSCNAL301唾液酸醛缩酶4.1.3.3N-Acetylneuraminic acid aldolase from MicroorganismActivity: >15 U/mg-Yellowish amorphous powderMw: 98,000-Store at -20 °CSCPCO301原⼉茶酸3,4双加氧酶1.13.11.3Protocatechuate 3,4-dioxygenase from Pseudomonas sp.Activity: >3 U/mg-Light brown amorphous powderMw: 700,000-Store at -20 °CSCPEO131过氧化物酶1.11.1.7Peroxidase from Horseradish, Grade IActivity: >250 U/mg-Reddish-brown amorphous powderMw: 40,000-Store at -20 °CSCPEO301过氧化物酶1.11.1.7Peroxidase from Horseradish, Grade I-Activity: >250 U/mgReddish-brown amorphous powder-Mw: 40,000-Store at -20°CSCPEO302过氧化物酶1.11.1.7Peroxidase from Horseradish, Grade III-Activity: >110 U/mgReddish-brown amorphous powder-Mw: 40,000-Store at -20°CSCPHO12C磷脂酶D Phospholipase D from Streptomyces chromofuscus3.1.4.4Activity: >40 U/mg-Brown amorphous powderMw: 57,000-Store at -20 °CSCPNP301嘌呤核苷磷酸化酶2.4.2.1Purine-nucleoside phosphorylase from MicroorganismActivity: >15 U/mg-White amorphous powderMw: 120,000-Store at -20 °CSCPPC301磷酸烯醇式丙酮酸羧化酶4.1.1.31Phosphoenolpyruvate carboxylase from Corn leavesActivity: >5 U/mg-White amorphous powderMw: 390,000-Store at -20 °CSCPSP101脯氨酸特定的肽链内切酶3.4.21.26Proline specific endopeptidase from Flavobacterium sp.Activity: >5 U/mg-White amorphous powder-Mw: 78,000-Store at -20 °CSCPYK302L丙酮酸激酶2.7.1.40Pyruvate kinase from Rabbit muscle-Activity:＞2000 U/mlwhite ammonium sulphate suspension-Mw:237000-Store at 2-8℃SCPYO311丙酮酸氧化酶1.2.3.3Pyruvate oxidase from Microorganism-Activity: >1.5 U/mgYellowish amorphous powder-Mw: 260,000-Store at -20 °CSCSAO341肌氨酸氧化酶1.5.3.1Sarcosine oxidase from Microorganism-Activity: >8 U/mgYellowish amorphous powder-Mw: 65,000-Store at -20 °CSCSAO351肌氨酸氧化酶1.5.3.1Sarcosine oxidase from Microorganism-Activity: >8 U/mgYellowish amorphous powder-Mw: 43,000-Store at -20 °CSCSOD302超氧化物歧化酶1.15.1.1Superoxide dismutase from Bovine erythrocyte-Activity: >3000U/mgBluish-green amorphous powder-Mw: 32,000-Store at -20 °CSCUAO201尿酸酶1.7.3.3Uricase from Candida sp.-Activity: >4 U/mg-White amorphous powder-Mw: 120,000-Store at -20 °CSCUAO211尿酸酶1.7.3.3Uricase from Bacillus sp.-Activity:>1.5 U/mg-White amorphous powder-Mw: 150,000-Store at -20 °CSCURH10S脲酶3.5.1.5Urease from Jack bean-Activity: >220 U/mg-White amorphous powder-Mw: 480,000-Store at -20 °CSCURH16C脲素酶GUrease G from Jack bean-Activity: >150 U/mgWhite amorphous powder-Mw: 480,000-Store at -20 °C3.5.1.5SCURH201脲素酶Urease from Jack bean-Activity: >100 U/mgWhite amorphous powder-Mw: 480,000-Store at -20 °C3.5.1.5SCXTO212黄嘌呤氧化酶Xanthine oxidase from Microorganism-Activity: >10 U/mgReddish-brown amorphous powder-Mw: 160,000-Store at -20°C1.1.3.222.诊断与研究⽤的辅酶CODES PRODUCTS CAS #SCADP01C 腺苷5'-⼆磷酸单钾盐⼆⽔合物ADP-K.2H2O-Adenosine 5’-diphosphate monopotasium saltdihydrate-C10H14N5O10P2K.2H2O-Mw:501.30-Colorless crystals-Purity:>95 %72696-48-1SCADP22C 腺苷5’-⼆磷酸⼆钠盐ADP-Na2-Adenosine 5’-diphosphate disodium salt-C10H13N5O10P2Na2-Mw:471.20-White powder-Purity:>98 %16178-48-6SCAMP02C 腺苷-5’-磷酸AMP-Adenosine 5’-monophosphoric acid-C10H14N5O7P.H2O-Mw:365.20-White powder-Purity:>98 %18422-05-4SCAMP05C 腺苷5’-磷酸AMP-Na2-Adenosine 5’-monophosphate disodium salt -C10H12N5O7PNa2-Mw:391.18-White powder-Purity:>95%18422-05-4SCATP03C 腺苷5’-三磷酸⼆钠盐3⽔合物ATP-Na2.3H2O-Adenosine 5’-triphosphate disodium salttrihydrate -C10H14N5Na2O13P3.3H2O -Mw:605.19-White powder-Purity:>96 %987-65-5SCBNA207C β-烟酰胺-腺嘌呤⼆核苷酸NAD-β-Nicotinamide-adenine dinucleotide-C21H27N7O14P2-Mw:663.4-White powder-Purity:>98 %53-84-9SCBND210C β-烟酰胺腺嘌呤⼆核苷磷酸，还原型四钠盐NADPH-Na4-β-Nicotinamide-adenine dinucleotide phosphate, reducedtetrasodium salt-C21H26N7O17P3.Na4-Mw:833.40-White powder-Purity:>93 %2646-71-1SCBNH208C β-烟酰胺腺嘌呤⼆核苷酸，还原⼆钠盐NADH-Na2-β-Nicotinamide-adenine dinucleotide, reduceddisodium salt -C21H27N7P2O14Na2-Mw:709.40-White to yellowish powder-Purity:>93 %606-68-8β-烟酰胺腺嘌呤⼆核苷酸磷酸⼆钠盐24292-60-2SCBNP209C β-烟酰胺腺嘌呤⼆核苷酸磷酸⼆钠盐NADP-Na2-β-Nicotinamide-adenine dinucleotide phosphatedisodium salt-C21H26N7O17P3Na2-Mw:787.40-Yellowishpowder-Purity:>97 %24292-60-2SCCOA11C 辅酶A三锂盐Coenzyme A trilithium salt-C21H33Li3N16O7P3S-Mw:785.40-White powder-Purity:>85 %18439-24-2SCDAD631C ⼆(腺苷-5’-)五磷酸三锂盐Ap5A-Li3-P1,P5 –Di(adenosine -5’-)pentaphosphate trilithiumsalt-C20H26N10O22P5Li3-Mw:934.20-Yellowish powder-Purity:>95 %75522-97-3SCFAD11C 黄素腺嘌呤⼆核苷酸⼆钠盐FAD- Na2-Flavine-adenine dinucleotide disodium salt-C27H31N9O15P2Na2-Mw:829.60-Orange powder-Purity:>93 %146-14-5SCNAL24C N-⼄酰-L-半胱氨酸N-Acetyl-L-cysteine-C5H9NO3S-Mw:163.20-White powder-Purity:>98 %616-91-1SASNAD 硫代辅酶IThio-NAD-C21H27N7O13SP2-Purity:≥ 90%4090-29-3SASNADP 硫代辅酶IIThio-NADP-C21H27N7O16P3S•Na- Purity:≥ 90%19254-05-8SAAldNAD 3-吡啶⼄醛腺嘌呤⼆核苷酸3-Pyridinealdehyde adenine dinucleotide C21H27N6O14P21986-7-7SAAC1023-⼄酰基吡啶腺嘌呤⼆核苷酸磷酸钠(Ac-NADP) APADP-C22H28N6O17P3•Na -Purity:≥ 80%102029-67-4SANAAD 烟酸腺嘌呤⼆核苷酸Nicotinic Acid Adenine Dinucleotide- C21H26N6O15P2104809-30-5SADeNAD 脱氨基NADDeamino Nicotinamide Adenine Dinucleotide-C21H26N6O15P2104809-38-3SAGGNAFB γ-L-⾕氨酰基-4-硝基苯胺Gamma-L-glutamyl-4-nitroanilide,-C11H13N3O5-Purity:≥ 96%7300-59-6SACGGN L-γ-⾕氨酸-(3-甲酸-4硝基苯胺)铵盐L-Glutamic Acid Gamma- (3-Carboxy-4-Nitroanilide),Ammonium Salt-C12H12N3O7P•NH4-Purity:≥ 96%63699-78-5SAPEPCHA 磷酸烯醇丙酮酸单环⼰胺盐PEP-C3H4O6P•C6H13N-Purity :＞95%10526-80-4SAPEPK 磷酸烯醇式丙酮酸单钾盐PEP-C3H4O6P•K-Purity :＞95%4265-07-03.诊断与研究⽤的底物CODES PRODUCTS CAS #SCAKE05C α–酮戊⼆酸⼆钠盐⼆⽔合物α–Ketoglutaric acid, disodium salt dihydrate-C5H4O5Na2.2H2O-Mw:226.10 -White powder-Purity:>98%305-72-6α–酮戊⼆游离酸328-50-7SCAKE115C α–酮戊⼆游离酸α–Ketoglutaric free acid-C5H4O5-Mw:146.10 -White powder-Purity:>99%328-50-7SCBTC06S-丁酰硫胆碱碘S-Butyrylthiocholine Iodide-C9H20NOSI-Mw:317.23 -White powder-Purity:>97%1866-16-6SCCNP005Gal-G2-α-CNP-C28H51O18Cl-Mw:659.98 -White powder-Purity:>90 %157381-11-8SCCRP59C 磷酸肌酸⼆钠盐四⽔合物Phosphocreatine disodium salt tetrahydrate-C4H8N3O5PNa2.4H2O-Mw:327.15 -White powder-Purity:>97 %19333-65-4SCGGC106C ⽢氨酰⽢氨酸Glycylglycine-C4H8N2O3-Mw:132.12-White powder-Purity:>98 %556-50-3SCGLT100L-⾕氨酸L-Glutamic acid-C5H9N2O4- Mw:147.13-White powder-purity:＞99%617-65-2SCGPS15C 葡萄糖-6-磷酸⼆钠盐Glucose-6-phosphate disodium salt-C6H11O9PNa2-Mw:304.20-White powder-Purity:>95 %3671-99-6SCLAC171C DL-乳酸锂盐DL-Lactic acid Lithium salt-C3H5O3Li-Mw:96.01-White powder-Purity:>95%16891-53-5SCLAL29C L-丙氨酸游离酸L-Alanine free acid-C3H7NO2-Mw:89.09-White powder-Purity:>99%56-41-7SCLAP41C L-天门冬氨酸L-Aspartic acid-C4H7NO4-Mw:133.10-White powder-Purity:>99 %56-84-8SCLAP42C L-天门冬氨酸,钠盐⼀⽔合物L-Aspartic acid, sodium salt monohydrate-C4H6NO4Na.H2O-Mw:173.10-White powder-Purity:>98 %323194-76-9SCLAP43C L-天门冬氨酸,镁⼆⽔合物L-Aspartic acid, magnesium salt dihydrate-C8H12N2O8Mg.2H2O-MW:324.50-White powder-Purity:>98 %2068-80-6SCLGC244C L-γ-⾕氨酰-3-羧基-4-硝基苯胺Glupa C-L-γ-Glutamyl-3-carboxy-4-nitranilide-C12H12N3O7NH4-Mw:328.30-Yellow powder-Purity:>99 %63699-78-5SCNAY138C 萘磷酸单钠盐Naphtyl phosphate, monosodium salt-C10H8NaO4P.H2O-Mw:264.15-White powder-Purity:>98%81012-89-7SCPG701C 亚⼄基降-4-硝基苯基-β-D-麦芽庚糖苷pNP-G7-Ethylidene-4-nitrophenyl-D-maltoheptaoside-C50H77NO38-Mw:1300.10-Yellowish powder-Purity:>90%96597-16-9对硝基苯基磷酸酯，⼆钠盐六⽔合物4264-83-9SCPNP264C 对硝基苯基磷酸酯，⼆钠盐六⽔合物PNPP-p-Nitrophenylphosphate, disodium salt hexahydrate-C6H4NO6PNa2.6H2O-Mw :371.10-White to yellow powder-Purity:>98%4264-83-9SCPNS265C p-硝基苯基磷酸酯，⼆tris盐PNPP diTris-p-Nitrophenylphosphate, ditris salt-C14H28N3O12P-Mw:461.40-White powder68189-42-4SCPYN100丙酮酸钠Sodium pyruvate-C3H3NaO3-Mw:110-White powder-Purity:>99%113-24-64.缓冲液Buffers for diagnostic & researchPRODUCTS CAS # N-(2-⼄酰胺基)-2-氨基⼄磺酸ACES-N-(2-Acetamido)-2-aminoethanesulfonic acid7365-82-4N-(2-⼄酰胺基)亚氨基⼆⼄酸ADA-(N-(2-Acetamido)iminodiacetic acid)26239-55-4 2-氨基-2-甲基-1-丙醇AMT -2-amino-2-methyl-1-propanol124-68-5 N,N-双(2-羟⼄基)-2-氨基⼄磺酸BES-N,N-Bis-(2-Hydroxyethyl)-2-Aminoethanesulfonic acid10191-18-1 N,N-双-(2-羟基⼄基)⽢氨酸Bicine-N,N-Bis-(2-Hydroxyethyl)glycine150-25-4 N-环⼰基-3-氨基丙磺酸CAPS-N-Cyclohexyl-3-aminopropanesulfonicacid1135-40-6N-环⼰基-2-羟基-3-氨基丙磺酸CAPSO -N-Cyclohexyl-2-hydroxy-3-aminopropanesulfonic acid73463-39-5。
VX-745_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:VX–745 is a potent and selective inhibitor of p38α, and possesses anti–inflammatory activity.In Vitro: VX–745 exhibits PBMC IL–1β and TNFα IC 50 values of 45 and 51 nM, respectively. VX–745 is also effective in whole blood,blocking IL–1β and TNFα release with IC 50 values of 150 and 180 nM, respectively. VX–745 shows a promising selectivity profile,with 20–fold selectivity for p38α over p38β (K i =220 nM)[1]. VX–745 solutions in DMSO/DMEM inhibits the IL–6 production with IC 50of 15±9 nM [2]. VX–745 (5.0 nM) displays potent activity and 1000–fold selectivity over closely related kinases, including ERK1,JNK1–3 and MK2. VX–745 (10 nM–50 μM) increasingly inhibits the anisomycin–induced activity of p38α[3]. VX–745 (0.06 μM–20 μM)inhibits IL–6 and VEGF secretion in BMSCs. VX–745 can inhibit cytokine (TNF–α, IL–6, VEGF)–induced paracrine MM cell growth,survival, and drug resistance in the BM microenvironment. VX–745 induces modest growth inhibition of MM.1S, RPMI8226, and U266 cell lines in a dose–dependent fashion, with inhibitory concentration of 50% (IC 50) of 10 μM [4].In Vivo: VX–745 (2.5, 5, and 10 mg/kg) improves the inflammatory scores in mice by 27%, 31%, and 44%, respectively [1]. VX–745(1.06 mg/kg) significantly decreases the inflammation score from 2.07±0.29 for the control group to 1.42±0.06[2].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]VX–745 inhibits p38α and p38β. The IC 50 for the inhibition of these two p38 homologs are obtained by aspectrophotometric coupled–enzyme assay. A fixed concentration of enzyme (15 nM of p38α or p38β) is incubated with various concentrations of VX–745 in DMSO for 10 min. at 30°C in 0.1 M HEPES buffer, pH 7.5, containing 10% glycerol, 10 mM MgCl 2, 2.5mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase, and 200 μM EGF receptor peptide. The reaction is initiated with 100 μM and 70 μM ATP for p38α and p38β assays, respectively. The decrease of absorbance at 340 nm is monitored to follow the rate of the reaction. IC 50 is evaluated from the rate data as a function of the inhibitor concentration.Cell Assay: VX–745 is dissolved in DMSO.[2]For these experiments, cells are plated at a density of 60,000 cells/well in 96–well plates.Each condition is tested in triplicate or more. The following day, all particle suspensions, active substances or control solutions are freshly prepared, distributed and incubated for 24 h at 37°C. Then, supernatants are carefully discarded. To perform the MTT test, 50μL of 0.1% MTT solution is added to each well for 3 h. Each well is then incubated for 1 h with 200 μL of dimethyl sulfoxide.Absorbance is measured at 595 nm. Reported results are expressed as the means±SD.Animal Administration: VX–745 is prepared in 100% propylene glycol.[1]Type II collagen–induced arthritis is established in male DBA/1mice with a minor modification. 10–Week old male DBA/1 mice are immunized by two intradermal injections within a 3 week interval using 100 μL of an emulsion consisting of a 1:1 (v/v) mixture of chick type II collagen (200 μg in 10 mM acetic acid) and complete Freund's adjuvant. Following the booster immunization, the mice are left untreated for 2–3 weeks, and are randomized into five treatment groups after they exhibit focal carpal (wrist) swelling (level 2 arthritic severity score) in both front paws. The five treatment groups are: 1: water control, 10 mL/kg, p.o., bid, (n=14); 2: 100% propylene glycol (PG) vehicle control, 10 mL/kg, p.o., bid, (n=8); 3:VX–745 in PG, at 10 mg/kg, p.o., bid, (n=7); 4: VX–745 in PG, at 5 mg/kg, p.o., bid, (n=10); and 5: VX–745 in PG, at 2.5 mg/kg, p.o., bid,Product Name:VX–745Cat. No.:HY-10328CAS No.:209410-46-8Molecular Formula:C 19H 9Cl 2F 2N 3OS Molecular Weight:436.26Target:p38 MAPK Pathway:MAPK/ERK Pathway Solubility:DMSO: 13.08 mg/mL (Need ultrasonic)(n=11). Arthritic symptoms are scored every other day using a level 1 to level 5 scoring system. Paw inflammation begins with erythema at the wrist (level 1), progressing to focal swelling of the wrist (level 2), to complete swelling of the wrist (level 3), to complete swelling of wrist and palm (level 4), and finally to complete swelling of wrist, palm and fingers (level 5). The sums of the scores from both front paw scores are used for plotting disease progression curves. Mice are sacrificed on day 20 and paws are removed, sectioned sagitally, stained with hemotoxylin & eosin, and scored for inflammation. Histologically, wrist joint inflammation begins with an infiltration of the synovium into the joint space (level 1), progressing to joint cartilage erosion (level 2), to joint cartilage and bone erosion (level 3), and finally to erosion of cartilage and bone accompanied by pannus formation (level 4). References:[1]. Duffy JP, et al. The Discovery of VX–745: A Novel and Selective p38α Kinase Inhibitor. ACS Med Chem Lett. 2011 Jul 28;2(10):758–63.[2]. Pradal J, et al. Intra–articular bioactivity of a p38 MAPK inhibitor and development of an extended–release system. Eur J Pharm Biopharm. 2015 Jun; 93:110–7.[3]. Bagley MC, et al. Rapid synthesis of VX–745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5107–10. Epub 2007 Jul 13.[4]. Hideshima T, et al. Targeting p38 MAPK inhibits multiple myeloma cell growth in the bone marrow milieu. Blood, 2003, 101(2), 703–705.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
低剂量普通肝素用于ECMO辅助支持患者抗凝治疗的系统评价
•临床评价-低剂量普通肝素用于ECMO辅助支持患者抗凝治疗的系统评价黄晓嫡，赵红卫，马永成，杜鹏强，倪铭，王爱凤(阜外华中心血管病医院药学部，河南郑州450000)［摘要］目的：系统评价低剂量普通肝素(UFH)用于体外膜肺氧合(ECMO)辅助支持患者的抗凝治疗。
方法：计算机检索PubMed、EMbase、Cochrane Library、CNKI、维普、万方和CBM数据库，纳入低剂量UFH用于ECMO辅助支持患者抗凝的回顾性队列研究。
根据NOS量表对纳入研究的质量进行评价。
采用RevMan5.3软件进行Meta分析。
结果：共计纳入5篇文献，包括469例患者，试验组(UFH低剂量)215例，对照组(UFH常规剂量)254例。
NOS评分为7~9分。
Meta分析结果显示，试验组和对照组的ECMO血管插管部位出血发生率分别为15.22%和40.74%,胃肠出血发生率分别为7.32%和14.62%,差异均有统计学意义(P<0.05);与对照组相比，试验组的压缩红细胞(PRBC)平均输注单位显著减少(P<0.01)o两组的手术部位出血、肺出血、颅内出血、血栓形成、ECMO撤机以及在院死亡率均无统计学差异(P>0.05)□结论：对于ECMO辅助支持患者，UFH调低剂量可减少ECMO血管插管部位和胃肠等部分出血事件，降低PRBC平均输注单位。
且尚无证据表明，调低UFH剂量会增加患者的血栓形成，延缓ECMO撤机，甚至提高在院死亡率。
受纳入研究质量及数量的限制，研究结果仍需更多大样本、高质量的研究加以验证。
［关键词］普通肝素；低剂量；体外膜肺氧合；抗凝；系统评价［中图分类号］R973+.2［文献标识码］A［文章编号］1672-8157(2020)06-0355-05Systematic review of the anticoagulant regimen of low-dose unfractioned heparin for patients on ECMOHUANG Xiao-jing,ZHAO Hong-wei,MA Yong-cheng,DU Peng-qiang,NI Ming,WANG A.i-feng(pepartment of Pharmacy,Fuwai Central China Cardiovascular Hospital,Zhengzhou450000,China)[ABSTRACT]Objective:To systematically review the anticoagulant regimen of low-dose unfractioned heparin(UFH)for patients on extracorporeal membrane oxygenation(ECMO).Methods:Databases including PubMed,EMbase,Cochrane Library, CNKI,VH\Wanfang and CBMdisc were searched for retrospective cohort studies about low-dose UFH used for patients on ECMO. Newcastle-Ottawa Scale(NOS)was used to evaluate the quality of the included studies.Meta-analysis was conducted by RevMan 5.3software.Results：A total of5cohort studies with a NOS score of7-9and469patients were included.There were215patients in experimental group(low-dose of UFH)and254patients in control group(routine dose of UFH).Results of meta-analysis showed that the rates of ECMO cannula site bleeding in experimental group and control group were15.22%and40.74%respectively,rates of gastrointestmal bleeding in the two groups were7.32%and14.62%respectively.There were significant dififerences between them(P <0.05).Compared with the control group,mean transfusion units of packed red blood cell(PRBC)markedly declined(P<0.01) in experimental group.Meanwhile,there were no statistical differences in rates of surgical site bleeding,pulmonary bleeding,cerebral bleeding,thrombosis,weaning of ECMO and in-hospital mortality between the two groups(P>0.05).Conclusion：For the patients on ECMO,low-dose UFH might help reduce the rates of cannula site bleeding,gastrointestinal bleeding,mean transfusion units of PRBC and had no influences on thrombosis,weaning of ECMO and the in-hospital mortality,which should be further proved by more studies with high quality due to the limitation of the quality and quantity of cohort studies involved in this study.[KEY WORDS]Unfractioned heparin;Low dose;Extracorporeal membrane oxygenation;Anticoagulation;Systematic review体外膜肺氧合(extracorporeal membrane［基金项目］吴阶平医学基金会临床药学专项基金(3206750190904)［通信作者］王爱凤，女，主任药师，研究方向：医院药学。
基因克隆实验流程
U PT OOF F40% 卓越速度 触手可及基因克隆实验流程特惠活动时间：2011年2月1日-4月30日特惠活动时间：2011年2月1日-4月30日© 2011 Roche Diagnostics LimitedS A LE如需订货或是了解本次活动详情，请联系我们免费订货热线: 800-820-3361 400-820-3361技术咨询: 800-820-0577 | *********************传真*************邮箱:******************更多优惠活动，请登陆罗氏网站查询/specials 本次活动最终解释权归罗氏应用科学部。
40% Off PCR 扩增试剂盒40% Off DNA 分离纯化试剂盒40% Off 克隆产品Up to 40% Off X-tremeGENE 转染试剂20% Off cOmplete ULTRA 蛋白酶抑制剂40% Off 逆转录产品上海市淮海中路1045号淮海国际广场12楼 邮编: 200031Tel: +86 21 3397 1000Fax: +86 21 3397 1188订货热线：800-820-3361 400-820-3361技术服务：800-820-0577|*********************邮箱：******************罗氏诊断产品(上海)有限公司罗氏应用科学部北京市东城区东长安街1号东方广场东方经贸城中二办公楼六层09室 邮编: 100738Tel: +86 10 8515 4100Fax: +86 10 8515 4188北京广州市环市东路403号广州国际电子大厦25楼邮编: 510095Tel: +86 20 8713 2600Fax: +86 20 8713 2700广州基因克隆实验流程手动核酸分离纯化目标核酸类型原始样本实验用时产量/得率推荐产品DNA 片段PCR 混合物, 限制性酶切产物, 琼脂糖凝胶切片, 经标记和修饰的反应混合物10 min5 -25 µg 大于 100 bp DNA 的回收率> 80% High Pure PCR Product Purification Kit 回收率> 85% ，最高可回收20 µg DNA High Pure PCR Cleanup Micro Kit 放射性标记的 DNA, 去除多余的荧光标记终止子7 min20 - 75 µl 标记混合物的回收率 > 80%mini Quick Spin DNA Columns质粒 DNA E. coli 质粒30 min2ml E. coli XL1菌液可分离pUC19质粒DNA 达 12 µg High Pure Plasmid Isolation Kit 60 min 30 ml E. coli DH5α 菌液可分离pBS 质粒DNA> 85 µg Genopure Plasmid Midi Kit 75 min150 ml E. coli XL1 blue 菌液可分离pUC19质粒DNA> 420 µgGenopure Plasmid Maxi Kit基因组DNA组织、培养细胞、细菌、酵母、血20 - 200 min ,取决于样本来源 3 - 20 µg ,取决于样本来源High Pure PCR Template PreparationKit哺乳类/人血1.5 hour ，不含重悬时间570 µg ，从10ml 鼠/兔全血浆中分离DNA Isolation for Mammlian Blood DNA 片段琼脂糖凝胶切片60 min0.4 - 9.5kb 的DNA 片断回收率为80%Agarose Gel DNA Extraction Kit产品选择指南更多信息，欢迎登录：/sis/napure核酸分离纯化■节省时间 – 更短的时间处理更多的样本。
化学仿制药参比制剂目录(第六十七批)
株式会社
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Pf Prism CV/UPJOHN US 2 LLC
未进口原研药品
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国际公认的同种药品
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蔗糖铁注射液
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BAXTER HEALTHCARE CORP
东洋纺织株式会社试剂说明书
manual THUNDERBIRD Probe qPCR Mix 0910 A4250K THUNDERBIRD™ Probe qPCR MixQPS-101T 1 mL x 1QPS-101 1.67 mL x 3Store at -20°C, protected from lightContents[1] Introduction[2] Components[3] Primer/Probe design[4] Template DNA[5] Protocol1. Standard reaction set up2. Cycling conditions2-1. Real-time PCR conditions using Applied Biosystems 7900HT2-2. Real-time PCR conditions using Roche LightCycler 1.1[6] Related ProtocolcDNA synthesis[7] Troubleshooting[8] Related productsC AUTIONAll reagents in this kit are intended for research purposes only. Do not use for diagnosis or clinical purposes. Please observe general laboratory precautions and observe safety procedures while using this kit.-LightCycler™ is a trademark of Idaho Technology, Inc. and Roche Molecular Systems, Inc.-TaqMan® is a registered trademark of Roche Molecular Systems, Inc.-SYBR® is a registered trademark of Roche Molecular Systems, Inc.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio 1JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************1[ 1 ] Introduction [ 2 ] Components DescriptionTHUNDERBIRD™ Probe qPCR Mix is a highly efficient 2x Master Mix for real-time PCR using TaqMan® probes. The master mix contains all required components, except for ROX reference dye, probe and primers (50x ROX reference dye is individually supplied with this kit). The master mix facilitates reaction setup, and improves the reproducibility of experiments.This product is an improved version of Realtime PCR Master Mix (Code No. QPK-101). In particular, reaction specificity and PCR efficiency is enhanced.Features-High specificityThe specificity for the detection of low-copy targets is improved.-Homogeneous amplificationThe dispersion of PCR efficiency between targets is reduced by a new PCR enhancer*. (*Patent pending)-Broad dynamic rangeHigh specificity and effective amplification enable the detection of a broad dynamic range.-Compatibility for various real-time cyclers.The reagent is applicable to most real-time cyclers (i.e. Block type and glass capillary type). Because the 50x ROX reference dye is individually supplied with this kit, the kit can be applied to real-time cyclers that require a passive reference dye.-Hot start PCRThe master mix contains anti-Taq DNA polymerase antibodies for hot start technology. The antibodies are easily inactivated in the first denaturation step, thereby activating the DNA polymerase.About the fluorescent probe detection systemThe TaqMan® probe system utilizes fluorescence emission from the probes. The probes hybridize to the target amplicons and then emit fluorescence upon degradation by the 5'-3' exonuclease activity of Taq DNA polymerase. This type of detection system can achieve higher specificity in real-time PCR assays than the SYBR® Green I detection system.This kit includes the following components for 40 reactions (QPS-101T) and 200 reactions (QPS-101), with 50 μl per reaction. All reagents should be stored at -20°C.<QPS-101T>THUNDERBIRD™ Probe qPCR Mix 1 ml x 150x ROX reference dye 50 μl x 1JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************2[ 3 ] Primer/Probedesign <QPS-101>THUNDERBIRD™ Probe qPCR Mix 1.67 ml x 350x ROX reference dye 250 μl x 1Notes:-THUNDERBIRD™ Probe qPCR Mix can be stored, protected from light, at 2-8°C for up to 3 months. For longer storage, this reagent should be kept at -20°C and protected from light. No negative effect was detected by 10 freeze-thaw cycles of THUNDERBRID™ Probe qPCR Mix. This reagent does not contain the ROX reference dye.-50x ROX reference dye can be stored, protected from light, at 2-8°C or -20°C. For real-time cyclers that require a passive reference dye, this reagent must be added to the reaction mixture at a concentration of 1x or 0.1x. The master mix solution with the ROX reference dye can be stored, protected from light, at 2-8°C for up to 3 months. For longer storage, this reagent should be kept at -20°C and protected from light. The pre-mixed reagents can be prepared according to the following ratios. [5] Table 1 shows the optimal concentration of the ROX dye.1x solutionTHUNDERBIRD™ Probe qPCR Mix : 50x ROX reference dye = 1.67 ml : 66.8 μl THUNDERBIRD™ Probe qPCR Mix : 50x ROX reference dye = 1 ml : 40 μl0.1x solutionTHUNDERBIRD™ Probe qPCR Mix : 50x ROX reference dye = 1.67 ml : 6.7 μl THUNDERBIRD™ Probe qPCR Mix : 50x ROX reference dye = 1 ml : 4 μlFor real-time cyclers that do not require a passive reference dye, THUNDERBIRD™ Probe qPCR Mix without the ROX reference dye can be used.1. Primer conditionsHighly sensitive and quantitative data depend on primer design. The primer should be designed according to the following suggestions;-Primer length: 20-30 mer-GC content of primer: 40-60%-Target length: ≤ 200 bp (optimally, 80-150 bp)-Melting temperature (Tm) of primers: 60-65°C-Purification grade of primers: Cartridge (OPC) grade or HPLC gradeNotes:-Longer targets (>200 bp) reduce efficiency and specificity of amplification.-Tm of the primers can be flexible, because the Tm value depends on the calculation formula.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************3[ 4 ] Template DNA 2. Fluorescent probeThe probes should be designed according to the guidelines of each probe system. Because insufficiently purified probes may inhibit the reaction, HPLC-grade probes should be used.The following DNA samples can be used as templates.1. cDNANon-purified cDNA, generated by reverse transcription reactions, can be used directly for real-time PCR using THUNDERBIRD™ Probe qPCR Mix. Up to 10% of the volume of a cDNA solution can be used for a real-time PCR reaction. However, excess volume of the cDNA may inhibit the PCR. Up to 20% (v/v) of the cDNA solution from ReverTra Ace® qPCR RT Kit (Code No. FSQ-101) can be used for real-time PCR (see [6]).2. Genomic DNA, Viral RNAGenomic DNA and viral RNA can be used at up to 200 ng in 50 μl reactions.3. Plasmid DNAAlthough super-coiled plasmids can be used, linearized plasmid DNA produces more accurate assays. The copy number of the plasmid DNA can be calculated by the following formula.Copy number of 1μg of plasmid DNA = 9.1 x 1011 / Size of plasmid DNA (kb)JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************4[ 5 ] Protocol1. Reaction mixture setupReaction volume FinalReagent50µl20µlConcentrationDWXµlXµlTHUNDERBIRD™ Probe qPCR Mix 25 µl 10 μl 1xForward Primer 15 pmol 6 pmol 0.3 μM*1Reverse Primer 15 pmol 6 pmol 0.3 μM*1TaqMan® Probe 10 pmol 4 pmol 0.2 μM*150x ROX reference dye 1μl / 0.1 μl 0.4μl / 0.04μl 1x / 0.1x*2DNA solution Y µl Y µlTotal50µl20µlNotes:*1 Primer / probe concentration should be determined according to the manufacturer’sinstructions.Higher primer concentration tends to improve the amplification efficiency, and lowerprimer concentration tends to reduce the non-specific amplification. The primerconcentration should be set between 0.2-0.6 μM.*2 50x ROX reference dye must be added when using real-time cyclers that require apassive reference dye, according to Table 1. Table 1 shows the optimum concentrationof the ROX reference dye. This dye is not necessary for real-time cyclers that do notrequire a passive reference dye.Table 1 Recommended ROX dye concentrationReal-time cycler Optimal dye concentration(dilution ratio)Applied Biosystems 7000, 7300, 7700, 7900HT etc. 1x (50:1)Applied Biosystems 7500, 7500Fast,Stratagene cyclers (Optional) etc.0.1x (500:1)Roche’ cyclers, Bio-Rad cyclers, BioFlux cyclers etc. Not requiredNotes:The ROX dye in Realtime PCR Master Mix (Code No. QPK-101) corresponds to 1xconcentration.JAPAN CHINA TOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140 www.toyobo.co.jp/e/bio********************52. PCR cycling conditionsThe following table shows the recommended thermal conditions using primers designed according to the recommended primer and probe conditions described in [3]. Almost all targets can also be amplified using the ongoing conditions with other real-time PCR reagents.*1Due to the anti-Taq antibody hot start PCR system, the pre-denaturation can be completed within 60 sec. The pre-denaturation time should be determined according to the recommendations of each real-time cycler. If the optimal pre-denaturation time cannot be determined, the time should be set at 60 sec.Table 2 The recommended pre-denaturation time for each real-time cycler Real-time cycler Pre-denaturation time High speed cycler (e.g. Applied Biosystems 7500Fast) 20 sec Capillary cycler (e.g. Roche LightCycler™ 1.x, 2.0) 30 secGeneral real-time cyclers (Applied Biosystems 7700, 7500,7900HT (normal block), Stratagene cyclers, BioFlux cyclers 60 sec *2The following table shows the optimal denaturation times for each real-time cycler. If the optimal denaturation time cannot be determined, the time should be set at 15 sec.Table 3 The recommended denaturation time for each real-time cycler Real-time cycler denaturation time High speed cycler (e.g. Applied Biosystems 7500Fast) 3 sec Capillary cycler (e.g. Roche LightCycler™ 1.x, 2.0) 5 secGeneral real-time cyclers (Applied Biosystems 7700, 7500,7900HT (normal block), Stratagene cyclers, BioFlux cyclers 15 sec *3Insufficient amplification may be improved by decreasing the extension temperature, and non-specific amplification (e.g. abnormal shapes of the amplification curve at low template concentrations) may be reduced by increasing the extension temperature. The extension temperature should be set at 56-64°C. *4If the target size is smaller than 300 bp, the extension time can be set at 30 sec on almost all real-time cyclers. Instability of the amplification curve or variation of data from each well may be improved by setting the extension time at 45-60 sec. Some real-time cyclers or software need over 30 sec for the extension step. In these cases, the time should be set according to each instruction manual (e.g. Applied Biosystems 7000/73000: ≥ 31 sec; Applied Biosystems 7500: ≥ 35 sec.).<3-step cycle> Temperature Time Ramp Pre-denaturation:95°C 20-60 sec *1Maximum Denaturation:95°C 1-15 sec *2 MaximumExtension: 60°C *3 30-60 sec *4 Maximum (data collection should be set at the extension step)JAPAN CHINA TOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140 www.toyobo.co.jp/e/bio********************62-1. Real-time PCR conditions using Applied Biosystems 7900HT(Normal block type, software version 2.2.2)The following is an example of a TaqMan ® assay using Applied Biosystems 7900HT.(1) The cycling parameters should be set according to the following “Thermal CyclerProtocol” window under the “Instrument” tab.Notes:- Appropriate sample volumes should be set. - ≥ 45 sec is necessary for the extension step.(2) Click the “Data collection” tab.(3) Insert the PCR plate(4) Start the programJAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************72-2. Real-time PCR conditions using Roche LightCycler 1.1(Software version 3.5)The following is an example of a TaqMan® probe assay using Roche LightCycler 1.1. (1)The cycling parameters should be set according to the following window. Analysisand Acquisition mode of the initial denaturation step must be set at “None”. (2)The cycling parameters should be set according to the following window. Analysismode of the PCR step must be set at “Quantification”. Acquisition modes of 95°C and 60°C must be set at “None” and “Single”, respectively.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************8(3)The cycling parameters should be set according to the following window. Analysisand Acquisition mode of the cooling step must be set at “Non”.(4) Insert the capillaries in the carousel, and start the cycling program.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************9[ 6 ] Related Protocol1. cDNA synthesiscDNA synthesized by various cDNA synthesis reagents can be used withTHUNDERBIRD™ Probe qPCR Mix. However, cDNA synthesized by a reagentspecialized for real-time PCR can increase sensitivity.ReverTra Ace® qPCR RT Kit (Code No. FSQ-101) is a cDNA synthesis kit suitable forreal-time PCR. Here, the protocol with ReverTra Ace® qPCR RT Kit is described.However, for the detailed protocol, please refer to the instruction manual of the kit.(1) Denaturation of RNAIncubate the RNA solution at 65°C for 5 min and then chill on ice.Notes:-This step can be omitted. But this step may increase the efficiency of the reversetranscription of RNA, which forms secondary structures.-Do not add 5x RT Buffer and/or enzyme solution at this step.(2) Preparation of the reaction solutionReagent V olume (amount)Nuclease-freeWaterXµl5x RT Buffer 2 µlPrimerMix 0.5µlEnzymeMix 0.5µlRNAsolution 0.5pg-1 µgTotal10µl(3) Reverse transcription reaction-Incubate at 37°C for 15 min. <Reverse transcription>-Heat at 98°C for 2 min. <Inactivation of the reverse transcriptase>-Store at 4°C or -20°C.**This solution can be used in the real-time PCR reaction directly or after dilution.Notes:The above temperature conditions are optimized for ReverTra Ace® qPCR RT Kit.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************10[ 7 ] TroubleshootingSymptom Cause SolutionLoss of linearity in the high cDNA/DNA concentration region. Inhibition by the components in thecDNA/DNA solution.-DNA: The DNA sample may contain PCRinhibitors. The DNA samples should berepurified.-cDNA: The components in the cDNA synthesisreagent may inhibit the PCR reaction. The cDNAsample should be used after dilution.The template DNA is insufficient. When the DNA/cDNA copy number is lower than10 copies per reaction, the linearity of the reactiontends to be lost. The template concentrationshould be increased.Adsorption of the DNA to the tubewall.The diluted DNA templates tend to be absorbedonto the tube wall. Dilution should be performedjust prior to experiments.Lost of linearity or lower signal in the lowDNA/cDNAconcentration region. Competition with primer dimerformation. In the probe assay, primer dimers are not detected. However, dimer formation may reduce the amplification efficiency of the target, especially for reactions at low template concentration. The reaction conditions should be optimized or the primer sequences should be changed.Loss of linearity of the amplification carves. Competition with non-specificamplification.In the probe assay, non-specific amplification isnot detected. However, non-specific amplificationmay reduce the amplification efficiency of thetarget. The reaction conditions should beoptimized or the primer sequences should bechanged.Inappropriate cycling conditions. Optimize the cycling conditions according to [5]. Degradation of the primers. Fresh primer solution should be prepared.The PCR efficiency is lower than 90% (slope:<-3.6) The calculation of the PCRefficiency is inappropriate. The Ct value on the linear region should be used to calculate PCR efficiency.The PCR efficiency is higher than 110%. The calculation of the PCRefficiency is inappropriate.The Ct value on the linear region should be usedto calculate PCR efficiency.Poor purification of the templateDNA.Low-purity DNA may contain PCR inhibitors.Re-purify the DNA samples.Absorption of the template DNA tothe tube wall.Diluted DNA templates tend to be absorbed ontothe tube wall. Dilution of the templateDNA/cDNA should be performed just prior toexperiments.Plasmid DNA or PCR product isused as a template.In general, plasmid DNA or PCR product is usedat low concentration. Diluted DNA templates tendto be absorbed onto the tube wall. Dilution of thetemplate DNA/cDNA should be performed justprior to experiments. Dilution with a carriernucleic acid solution (Yeast RNA) is alsoeffective in improving linearity.Inappropriate thermal conditions. Optimize the thermal conditions according to [5].Reproducibility is notgood.Low purity of the primers or probes.Different lots of primers or probes may showdifferent results. When the lot is changed, priortesting of the primer or probe should beperformed.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************11Symptom Cause SolutionContamination or carry over of the PCR products. Change the contaminated reagent.Amplification from the non-template control(NTC). Inappropriate settings offluorescence measurement, such asin the case of multiplex PCR. In multiplex experiments, inappropriate setting of fluorescence measurement may cause the detection of noise by the cross talk of fluorescent dyes. Settings should be reconfirmed.Excessive amount of ROX reference dye. Excessive amount of ROX reference dye may cause low signal. 50x ROX reference dye should be used according to [5] Table 1.Inappropriate settings of fluorescence measurement. Settings should be confirmed according to the instruction manual of each detector.Low purity of fluorescent probes. Low purity of the probe may increase the baseline. HPLC grade probes should be used.Excessive intensity of the quencher Dye. Certain quenchers (e.g. TAMRA) may cause a higher baseline because of its fluorescence. Use of a non-fluorescent quencher may improve the high baseline.Degradation of the probe. Store the probes according to the manufacture’srecommendations.Insufficient fluorescence measurement time. Certain detection systems require a longer time to detect the fluorescent signal. Longer extension (measurement) time (45-60 sec) may improve the unstable signal.Low amplificationcurve signal /Unstable amplificationcurve signal.Insufficient reaction volume. Low reaction volume may cause an unstablesignal. Increase the reaction volume.JAPAN CHINATOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140www.toyobo.co.jp/e/bio********************12[ 8 ] Related productsProduct name Package Code No.High efficiency real-time PCR master mix THUNDERBIRD™ SYBR® qPCR Mix 200reactionsQPS-201High efficiency cDNA synthesis kit for real-time PCR ReverTra Ace® qPCR RT Kit 200reactionsFSQ-101One-step Real-time PCR master mix for probe assayRNA-direct™ Realtime PCR Master Mix 0.5 mL x 20.5 mL x 5QRT-101TQRT-101One-step Real-time PCR master mix for SYBR® Green assayRNA-direct™ SYBR® Realtime PCR Master Mix 0.5 mL x 20.5 mL x 5QRT-201TQRT-201JAPAN CHINA TOYOBO CO., LTD. TOYOBO Bio-Technology, CO., LTD.Tel(81)-6-6348-3888 Tel(86)-21-58794900.4140 www.toyobo.co.jp/e/bio********************NOTICE TO PURCHASER: LIMITED LICENSEA license to perform the patented 5’ Nuclease Process for research is obtained by the purchase of (i) both Authorized 5' Nuclease Core Kit and Licensed Probe, (ii) a Licensed 5’ Nuclease Kit, or (iii) license rights from Applied Biosystems.This product is an Authorized 5’ Nuclease Core Kit. Use of this product is covered by one or more of the following US patents and corresponding patent claims outside the US: 5,079,352, 5,789,224, 5,618,711, 6,127,155, 5,677,152, 5,773,258, 5,407,800, 5,322,770, 5,310,652, 5,210,015, 5,487,972, and claims outside the US corresponding to US Patent No. 4,889,818. The purchase of this product includes a limited, non-transferable immunity from suit under the foregoing patent claims for using only this amount of product for the purchaser’s own internal research. Separate purchase of a Licensed Probe would convey rights under the applicable claims of US Patents Nos. 5,538,848, 5,723,591, 5,876,930, 6,030,787, 6,258,569, 5,804,375 (claims 1-12 only), and 6,214,979, and corresponding claims outside the United States. No right under any other patent claim and no right to perform commercial services of any kind, including without limitation reporting the results of purchaser's activities for a fee or other commercial consideration, is conveyed expressly, by implication, or by estoppel. This product is for research use only. Diagnostic uses under Roche patents require a separate license from Roche. Further information on purchasing licenses may be obtained from the Director of Licensing, Applied Biosystems, 850 Lincoln Centre Drive, Foster City, California 94404, USA.。
SNS-032_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:SNS–032 is a selective inhibitor of cyclin–dependent kinase (CDK), inhibiting CDK2/7/9 with IC 50s of 48 nM/62 nM/4 nM.IC50 & Target: IC50: 48 nM (CDK2), 62 nM (CDK7), 4 nM (CDK9)In Vitro: SNS–032 has low sensitivity to CDK1 and CDK4 with IC 50 of 480 nM and 925 nM, respectively. SNS–032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS–032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS–032 activity is readily reversible; removal of SNS–032 reactivates RNA polymerase II, which led to resynthesis of Mcl–1 and cell survival [1].SNS–032 inhibits three dimensional capillary network formations of endothelial cells. SNS–032 completely prevents U87MGcell–mediated capillary formation of HUVECs. In addition, SNS–032 significantly prevents the production of VEGF in both cell lines,SNS–032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS–032 induces cell cycle arrest and apoptosis across multiple cell lines [2]. SNS–032 blocks the cell cycle via inhibition of CDKs 2and 7, and transcription via inhibition of CDKs 7 and 9. SNS–032 activity is unaffected by human serum [3]. SNS–032 induces a dose–dependent increase in annexin V staining and caspase–3 activation. At the molecular level, SNS–032 induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 anddephosphorylated CDK7[5].In Vivo: SNS–032 (15 mg/kg, i.p.) inhibits both xenografted BaF3–T674I cells and KBM5–T315I cells in vivo. SNS–032 abrogates the growth of tumors transplanted in nude mice with downregulation of T674I PDGFRα and T315I–Bcr–Abl [4].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[2]Cell Titer–Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs andU87MG cells. U87MG cells and HUVECs (2×103 cells/well) are seeded in a 96–well microplate in a final volume of 100 mL. After 24hours, cells are treated with various doses of SNS–032 (0–0.5 mM) for 24, 48, or 72 hours. After completion of the treatment, 100 mL of CTG solution is added to each well and incubated for 20 minutes at room temperature in the dark. Lysate (50 mL) is transferred to a 96–well white plate, and luminescence is measured by POLARstar OPTIMA. Percent cell growth is calculated by considering 100%growth at the time of SNS–032 addition.Animal Administration: SNS–032 is dissolved in tissue culture grade DMSO. [4]Nude nu/nu BALB/c mice are housed in barrier facilities with a 12–hour light–dark cycle, with food and water available ad libitum. A mixture of 1×107 of BaF3–T674I cells withMatrigel or KBM5–T315I cells (3×107) are inoculated subcutaneously on the flanks of 4– to 6–week–old male nude mice.Tumors are measured every other day with use of calipers. Tumor volumes are calculated by the following formula: a 2×b×0.4,where a is the smallest diameter and b is the diameter perpendicular to a. Four days after subcutaneous inoculation, when tumors are palpable (appr 100 mm 3), mice are randomized to receive treatment with vehicle (tissue culture medium containing DMSO 0.1%v/v) or SNS–032 (15 mg/kg injected intraperitoneally every 2 days) for about 2 weeks. SNS–032 is dissolved in tissue culture gradeProduct Name:SNS–032Cat. No.:HY-10008CAS No.:345627-80-7Molecular Formula:C 17H 24N 4O 2S 2Molecular Weight:380.53Target:CDK Pathway:Cell Cycle/DNA Damage Solubility:10 mM in DMSODMSO before dilution. The body weight, feeding behavior, and motor activity of each animal are monitored as indicators of general health. The animals are then euthanized, and tumor xenografts are immediately removed, weighed, stored, and fixed.References:[1]. Chen R, et al. Mechanism of action of SNS–032, a novel cyclin–dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637–45.[2]. Ali MA, et al. SNS–032 prevents tumor cell–induced angiogenesis by inhibiting vascular endothelial growth factor. Neoplasia. 2007 May;9(5):370–81.[3]. Conroy A, et al. SNS–032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep;64(4):723–32.[4]. Wu Y, et al. Cyclin–dependent kinase 7/9 inhibitor SNS–032 abrogates FIP1–like–1 platelet–derived growth factor receptor α and bcr–abl oncogene addiction in malignant hematologic cells.Clin Cancer Res. 2012 Apr 1;18(7):1966–78. Epub 2012 Mar 23.[5]. Walsby E, et al. The cyclin–dependent kinase inhibitor SNS–032 has single agent activity in AML cells and is highly synergistic with cytarabine.Leukemia. 2011 Mar;25(3):411–9. Epub 2011 Jan 7.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
211212207_熟地黄炮制过程中的化学成分变化和药理作用研究进展
2023年第3期品牌与标准化Prepared Radix Rehmanniae Research Progressin Chemical Composition Changes and Pharmacological EffectsGENG Xiaotong（Xinyang Agricultural and Forestry University 〔School of Pharmaceutical Engineering 〕，Xinyang 464000，China ）Abstract ：In this paper ，the processing methods of Radix Rehmanniae Preparata and the representative research results of the changes of its chemical components before and after are reviewed.Its main changes include iridoid and its glycosides ，phenylethanolamine glycosides and 5-HMF ，carbohydrates and others.Its main effects include improving the immune system ，blood system ，inhibiting tumor growth ，etc.Key words ：rehmanniae radix praeparata ；processing method ；chemical composition ；pharmacological action熟地黄炮制过程中的化学成分变化和药理作用研究进展耿晓桐（信阳农林学院〔制药工程学院〕，河南信阳464000）【摘要】本文对熟地黄的炮制方法和化学成分前后变化的代表性研究成果进行综述，其主要变化成分包括环烯醚萜及其苷类、苯乙醇苷类和5-HMF ，糖类以及其他，主要功效包括改善免疫系统、血液系统、抑制肿瘤生长等。
4,4′-二异氰酸酯二环己基甲烷 核磁氢谱
4,4'-二异氰酸酯二环己基甲烷核磁氢谱（四氢基二异氰酸酯）也叫四氢基二异氰酸酯，是一种重要的有机化合物。
它的核磁氢谱是对这种化合物进行结构分析的关键工具之一。
1. 介绍与基本信息4,4'-二异氰酸酯二环己基甲烷，化学式(C7H8N2O2)x (C6H10O4)y，分子量 319.0。
四氢基二异氰酸酯是通式为C7H8N2O2的异氰酸酯类化合物的一种。
它有多种同分异构体，其中4,4'-二异氰酸酯二环己基甲烷是常见的一种。
2. 核磁氢谱的含义核磁共振（NMR）是一种通过核自旋产生共振现象的物理方法，用于获得某种化合物分子的信息，包括化学成分、结构和环境。
核磁氢谱是一种常用的核磁共振谱谱图，用于分析化合物中氢原子的信息。
通过核磁氢谱的峰位和峰型可以推断出化合物分子中氢原子所处的化学环境，从而揭示出分子的结构特征。
3. 深入探讨核磁氢谱在四氢基二异氰酸酯分子中，氢原子的化学环境有着特定的分布和取向，因此其核磁氢谱是多峰的。
通过对核磁氢谱峰位的解读和分析，可以推断出四氢基二异氰酸酯分子中不同环境下的氢原子，并据此反推出分子的结构。
4. 总结与展望总体来说，核磁氢谱是一种非常重要的化学分析工具，对于研究和分析有机化合物的结构有着至关重要的作用。
通过对四氢基二异氰酸酯核磁氢谱的研究，不仅可以了解其结构特征，还可以为其在不同领域的应用提供技术支持。
在未来，随着核磁共振技术的不断发展，相信核磁氢谱在有机化合物领域的研究中会发挥越来越重要的作用。
对于核磁氢谱和四氢基二异氰酸酯的个人理解是，核磁共振技术的提出和发展为化学研究和工业生产提供了强有力的工具和支持。
而四氢基二异氰酸酯作为有机化合物中的重要代表，在其结构分析中核磁氢谱则发挥着关键的作用，有助于我们更深入地了解其结构特征和化学性质。
希望通过本文的介绍和探讨，读者能对核磁氢谱和四氢基二异氰酸酯有更全面、深入的了解。
在我提供的文章主题框架下，我会着手撰写一篇深度和广度兼具、高质量的中文文章，以满足你的要求。
CFI-402257-SDS-MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Oct.-06-2018Print Date:Oct.-06-20181. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :CFI-402257Catalog No. :HY-101340CAS No. :1610759-22-21.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:CFI402257;CFI 402257Formula:C28H30N6O3Molecular Weight:498.58CAS No. :1610759-22-24. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2018 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
疏血通与丹参注射液配伍丹参活血汤治疗下肢静脉血栓的临床观察
疏血通与丹参注射液配伍丹参活血汤治疗下肢静脉血栓的临床观察发表时间：2018-03-01T11:32:49.023Z 来源：《医药前沿》2018年1月第2期作者：孟哲民[导读] 疏血通与丹参注射液并用配合丹参活血汤治疗下肢静脉血栓临床效果较疏血通配伍丹参注射液有效率更高。
（沈阳铁西恩泽中医院辽宁沈阳 110020）【摘要】目的：探讨疏血通注射液与丹参注射液并用配合丹参活血汤治疗下肢静脉血栓的的临床疗效。
方法:回顾性分析30例下肢静脉血栓患者的临床资料,将其随机分为治疗组和对照组各15例。
对照组患者采用疏血通注射液配合丹参注射液治疗，治疗组患者在对照组治疗的基础上加中药汤剂“丹参活血汤”治疗,比较两组患者的治疗效果。
结果:治疗组患者总有效率为100.0%,优于对照组总有效率为86.7%,差异具有统计学意义（P＜0.05）。
结论：疏血通与丹参注射液并用配合丹参活血汤治疗下肢静脉血栓临床效果较疏血通配伍丹参注射液有效率更高，值得临床推广应用。
【关键词】疏血通注射液；丹参注射液；下肢静脉血栓；丹参活血汤；D二聚体检测。
【中图分类号】R274.9 【文献标识码】B 【文章编号】2095-1752（2018）02-0349-02 下肢静脉血栓中医名称相当于“股肿”，是由于下肢深部静脉血栓形成和炎性病变引起的一种疾病，是一种急性非化脓性炎症。
一般多发生在下肢并伴有即发性血管内血栓形成的疾病，病变主要累积四肢或表静脉或下肢混静脉，其临床特点为患肢局部肿胀、疼痛，皮下可扪及有压疼的条索状或伴有病变远端表浅静脉曲张等静脉回流受阻现象，患肢局部皮温升高四大症状，本病好发于下肢髂静脉和股静脉，也可因血栓脱落而造成肺栓塞而危及生命[1]。
临床表现：最常见的主要临床表现是一侧肢体的突然肿胀，患者下肢深静脉血栓形成的患者局部疼痛，行走时加剧，轻者局部仅感沉重，站立时症状加重，大腿内侧三角区有明显压痛，肿胀疼痛、胫足水肿、皮温升高、皮肤增厚、色素沉着[2]。
CDU-550 Modem User Guide.pdf_1697677138.353466说明书
Test Report No.: NK2GR079CMOTech Co., Ltd.FCC ID :TARCDU-550Page 66 of 68Appendix F – USER’S ManualCDU-550 Modem User GuideFCC RF EXPOSURE COMPLIANCEIn August 1996 the Federal Communications Commission (FCC) of the United States with its action in Report and Order FCC 96-326 adopted an updated safety standard for human exposure to radio frequency (RF) electromagnetic energy emitted by FCC regulated transmitters. Those guidelines are consistent with the safety standard previously set by both U.S. and international standards bodies. The design of this modem complies with the FCC guidelines and these international standards.Use only the supplied or an approved antenna. Unauthorized antennas, modifications, or attachments could impair call quality, damage the modem, or result in violation of FCC regulations. This CDMA 1xEVDO USB data modem has been tested for FCC RF exposure hand and body SAR compliance with the CDU-550 USB dongle modem form factor. In order to comply with FCC RF exposure requirements, the CDMA 1xEVDO USB data modem must be operated with the CDU-550 USB dongle modem form factor. The use of this device in any other type of host configuration may not comply with FCC RF exposure requirements and should be avoided. During operation, a1.5cm separation distance should be maintained between the antenna, whether extended or retracted, and the user’s/bystander’s body (excluding hands, wrists, feet, and ankles) to ensure FCC RF exposure compliance.CAUTIONChange or modification to the modem without the express consent of Data Poz Co., Ltd. voids the user’s authority to use the equipment. This equipment has been tested and found to comply with the limits pursuant to Part 22 of the FCC rules. These limits are designed to provide reasonable protection against harmful interference in an appropriate installation. This equipment generates, uses, and can radiate radio frequency energy and, if not used in accordance with instructions, can cause harmful radiation to radio communication. However, there is no guarantee that interference will not occur in a particular installation. If the equipment does cause harmful interference in radio and television reception, which can be determined by turning the equipment on and off, the user is encouraged to try to correct the interference by one or more of the following measures:■ Reorient or relocate the receiving antenna■ Increase the separation distance between the equipment and the receiver■ Connect the equipment into an outlet on a circuit different from that to which the receiver is connected.■ Consult the dealer or an experienced Radio / TV technician for help.This equipment has been tested and found to comply with the limits for a class B digital device, pursuant to Part 15 of the FCC rules. These limits are designed to provide reasonable protection against harmful interference in a residential installation. This equipment generates, uses, and can radiate radio frequency energy and, if not installed and used in accordance with the instructions, may cause harmful interference to radio communication. However, there is no guarantee that interference will not occur in a particular installation. If this equipment does cause harmful unacceptable interference to radio and television reception, which can be determined by turning the equipment on and off, the user is encouraged to try to correct the interference by one or more of the following measures:■ Reorient or relocate the receiving antenna■ Increase the separation distance between the equipment and the receiver■ Connect the equipment into an outlet on a circuit different from that to which the receiver is connected.■ Consult the dealer or an experienced Radio/TV technician for help.Cautions for Users-Use of CDU-500 EV-DO Modem (hereinafter referred as modem ), while running a notebook PC with a battery, may cause earlier exhaustion of the battery than usual due to additional consumption of electric currents.-Be cautious when you touch a modem with a bare hand after long use, it may cause a burn due to its high temperature. Pick it out with the antenna after separation.-Do not allow children or pets to approach or touch the modem when separated from a notebook PC or PDA.-Do not give impact to the modem or throw it away.-Use the leather case provided along with the modem when you carry the modem.-When the modem is lost or stolen, immediately report it to the corresponding telecommunication operator.-Do not recklessly lend your own modem to anybody else.-Call to a service center designated by CMOTech for after-sales service.-Do not attach an additional device which may cause alteration in performance of the product registered for the type approval.-This modem sends and receives the radiofrequency (RF) energy in status of power-on. The radiofrequency (RF) energy may affect a human body.-Use an antenna only approved by CMOTech. Otherwise it may cause a damage on the modem and you will not get a free after-sales service.-Use the modem in the manner you use a notebook PC in general.-Make the antenna stand and do not touch it when being used. If the antenna is touched, the quality of transmission and reception may be lowered and it will cause excessive power consumption.-Be cautious as the radiofrequency (RF) energy may affect the electronic devices installed in a car. -Be noticed that most of electronic devices are designed to be free from the RF energy but there are some products that may be out of order due to the RF energy.-Medical Devices Industry Association recommends the patients using a pacemaker not to use RF using devices such as cell phones, wireless modems and so on because using those devices in the range of 15cm from the pacemaker may affect the pacemaker. In an inevitable situation, make it sure to keep the distance of more than 15cm between the modem and the pacemaker. To minimize the possible interference, use the modem on the opposite side of the pacemaker. Do not use it if possible.-If you use a medical device, ask the manufacturer if the device is free from the RF energy. Some hospitals use RF medial devices. Separate the modem from a notebook PC or a PDA when entering a hospital.-The modem may affect the functions of a hearing-aid.-The places banning use of cell phones may require prohibit use of modems.-Separate the modem from a notebook PC or PDA we you get on an airplane.-Separate the modem from a notebook PC or PDA to avoid interference with explosive operations at a blasting area or a place posted Turn off a walkie-talkie . And follow all the instructions shown in the area.-Hold yourself in installing or using the modem at the places such as danger areas of gas leakage, chemical storage facilities, decks of a vessel and so on. Sparks may occur when you install the modem onto a notebook PC or a PDA on rare occasions.CDU-550 Modem InstallSetupInsert installation CD (supplied with CMOTech Data Modem) into the CD-ROM drive.This will automatically start the installation and install the required drivers plus CMOTech Data Modem Application software.Do not connect CMOTech Data Modem into your laptop/PC yet.The installation procedures are the Windows 2000 and Windows XP.Start setupIf the auto run does not start after inserting the CD, please double-click on Setup.exe file on CD-ROM to start the installation.If you have already inserted your Modem into your PC, remove the Modem and double-click Setup.exeStart Auto RunInstall Shield Wizard... click 'next'Choose the installation directory and click "Next" to continue.Click "Install" to continue.CMOTech Modem is configuring your new software installation. Copying Step1 FileCopying Step2 FileCheck deviceInstallation Complete. Click Finish and remove the installation CD.Insert ModemPlease Insert ModemOn Window 2000As inserting Modem on Window 2000, there will not be any window and users can run applications after the device is detected.On Window XPIf your operation system is XP on inserting Modem, you can see Find New Hardware Dialog. Step 1 - Data Modem @ CDMA Composite Device InstallStep 2 - Data Modem @ CDMA(5553) InstallStep 3 - Data Modem @ CDMA Diagnostic Serial Port(WDM)(5553) InstallModem Driver Install FinishUsing the CDU-550 Modem Application Software During this installation a Shortcut will have been placed on your desktop for the CMOTech Data Modem Application software.Note : If the modem is connected to the Laptop/PC via serial port, the user will have to select the serial portinitially when the User Interface software starts up.On auto start of the Application Software, the first screen you will see Main window.Activate your CMOTech Connection modemSetting SPCSetting MIN / MDNThe modem will be rebooted.MainIndicator state IconsIconMeaningIconMeaningNo SignalRoamingAntenna / Signal StrengthCoverage Icon. CDMA 1x availableCurrent High Data Rate mode selected : Hybrid Mode(1xEV-DO Preferred) DEFAULT. The modem will automatically look for the highest speednetwork available in this mode.Coverage Icon. IS95 available onlyCurrent High Data Rate mode selected: CDMA 1X only ModeCoverage Icon. 1xEV-DO availableCurrent High Data Rate mode selected: 1xEV-DO only Mode.Active Data connectionDormant Data connectionTaskbar IconWhen the Application Software is running in the background, the Windows taskbar will show an icon as above.To maximize the Application Software, double click on the icon.Dial up NetworkConnectionClicking the Connect button. The Application Software will start dialing the Service Option selectedunder dial-up when the Connect button is clicked (The Connect button can be clicked on the main window).Verifying User.Registering your computer on the network.You can see above window s right blue icon. This icon show on connection.Warning : If you install Windows XP service pack 2, you must turn off firewall in Window security center.If you try connecting with turn on firewall, you can see connecting fail.Click the Windows taskbar's shield - shaped Yellow icon, you can see Window Security center To DisconnectClicking the disconnect button on the Main window or Dial up slide window, will disconnect the dialup connection and the modem will switch to idle mode.Clicking the Yes button.Active and Dormant stateIt is on Active state when an active icon appears on the window.If having no data transmission during Dialup, it goes to Dormant state.Users can discern that it is on Dormant state with an icon displayed on the screen.OptionGeneralNOTE : The Apply button must be clicked for any changes to take effect.Application Software auto run : This Check box determines whether the Application Software starts automaticallywhen the Modem is connected. Check the check box and press Apply button.Hibernation : With the Application Software running (idle). Windows will not hibernate or switch to standby mode.Please select this option under General tab to close UI automatically so that windows can hibernate or switch to standby.DataConnection settingTo Setting Dial-Up connection, click Option button and click Data button.Also to change connecting type, click the radio Button.NOTE : You can use Packet, QNC type in 1X current coverage. And can t use Packet type in IS 95 coverage.Connecting is also possible to connect (Dial-up) by clicking the connect button on the main window without openingthe Dial-up setting window. When clicking the connect button, the last Service option will be used for dial up.If the user changes the username or password and clicks Connect, the Application Software will store the new username and password.To load the The default username and password select the Restore button, and the Apply button must be clicked.Dial-up Networking - PacketAlways On is a CDMA 1x internet domain that applies to data (in Kilobytes) based charging packages.This service allows you to remain connected to the internet all the time.charges will apply to the amount of data sent and received with this domain.Dial-up Networking - QNC Standard.When you are not within CDMA 1x coverage or you have not subscribed to CDMA 1x, you can still connect tooperator's Standard Mobile internet Service using Quick Net Connect, provided you are withis CDMA coverage.Quick Net Connect (QNC) does not require a separate subscriptionAboutIt displays Software/ Firmware Version, PRL ID as shown below.Data LogsData LogsThe User Data Counter will continuously accumulate on each session and will only clear when Clear Data Count is clicked.UninstallUninstall CMOTech CDU-550 ModemTo uninstall CMOTech CDU-550 Modem driver, click Uninstall . Start uninstallExecute the Uninstall program.Execute setup.exe in installation folder or click UninstallAuto RunPress buttonAs clicking Uninstall icon, you can see a dialog below. Click yes button.Uninstall continue.Uninstall program remove file in your PC. (Uninstall Program deletes Drivers, Modem and Modem Application Program.)Uninstall Complete. Click Finish button.。
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Inhibitors, Agonists, Screening Libraries
Data Sheet
BIOLOGICAL ACTIVITY:
CFI–402257 is a highly selective and orally bioavailable TTK and Mps1 inhibitor with K i s of 0.1 and 0.09 nM, respectively.
IC50 & Target: Ki: 0.1 nM (TTK)[1], 0.09 nM (Mps1)[2]; EC50: 6.5 nM (Mps1)[2]
In Vitro: CFI–402257 is highly selective to TTK. CFI–402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI–402257 is a potent inhibitor of cell growth [1]. CFI–402257 shows strong antineoplastic activity on a broad panel of human cancer–derived cell lines, and causes effects consistent with depletion or inhibition of Mps1. CFI–402257 inhibits Mps1 with an IC 50 value of 1.2 nM, and is ATP competitive with a K i value of 0.09 nM. CFI–402257 inhibits autophosphorylation of Mps1 at threonine 12/serine 15 with an EC 50 value of 6.5 nM in cells exogenously expressing human Mps1. CFI–402257 exerts potent growth inhibitory activity across the vast majority of cell lines with a median IC 50 value of 15 nM [2].
In Vivo: The upper dose level for once–daily administration of CFI–402257 is between 6 and 6.5 mg/kg. CFI–402257 given orally QD shows dose–dependent activity in mice with established tumors from xenografted MDA–MB–231 human TNBC cells [5 mg/kg
CFI–402257, tumor growth inhibition (TGI)=74%; 6 mg/kg, TGI=89%], from xenografted MDA–MB–468 human TNBC cells in mice (5mg/kg, TGI=75%; 6 mg/kg, TGI=94%). CFI–402257 also demonstrates antitumor activity in a platinum–resistant PDX model of high–grade serous ovarian cancer (6.5 mg/kg, TGI=61%). CFI–402257 is found to be similarly efficacious in a platinum–sensitive PDX model of high–grade serous ovarian cancer [2].
PROTOCOL (Extracted from published papers and Only for reference)
Cell Assay: CFI–402257 is prepared as 10 mM stocks in 100% DMSO and diluted with DMEM containing 10% (vol/vol) FBS.[2]Cells are treated with 20 pM to 10 μM CFI–402257 for 5 days. After 5 d, cell growth in each well is assessed by an SRB assay. SRB absorbance values are adjusted by subtracting the average of the baseline readings from untreated cells assessed 1 d after cell seeding. Relative cell growth is calculated by comparing vs. DMSO–treated cells. The concentrations at which cell growth is inhibited by 50% are calculated by using GraphPad Prism software [2].
Animal Administration: CFI–402257 is prepared in 10% (vol/vol) NMP/40% (vol/vol) PEG–300/50% (vol/vol) water for the
hydrochloride form, or 80–90% (vol/vol) PEG–300 or PEG–400/20–10% (vol/vol) water for the bisphosphate hemihydrate
form.[2]Mouse: CFI–402257 and the vehicle are administered by oral gavage, and carboplatin, anti–PD–1 antibody, and isotype control are administered by i.p. injection to mice as described earlier. Animal weights are monitored daily, and tumor volume is measured three times per week [2].
References:
Product Name:
CFI–402257Cat. No.:
HY-101340CAS No.:
1610759-22-2Molecular Formula:
C 28H 30N 6O 3Molecular Weight:
498.58Target:
Mps1; Mps1Pathway:
Cell Cycle/DNA Damage; Cytoskeleton Solubility:
DMSO: 10 mM (Need Warming and Ultrasonic)
[1]. Liu Y, et al. Discovery of Pyrazolo[1,5–a]pyrimidine TTK Inhibitors: CFI–402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671–5.
[2]. Mason JM, et al. Functional characterization of CFI–402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127–3132.
Caution: Product has not been fully validated for medical applications. For research use only.
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