蒽环类抗生素Idarubicin抑制DNA拓扑异构酶II (topo II)CAS号58957-92-9生物活性

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生物活性 Idarubicin是蒽环类抗生素,抑制DNA拓扑异构酶II (topo II),作用于MCF-7细胞,IC50为3.3 ng/mL。
实验操作 来自于公开的文献,仅供参考
细胞实验 细胞系 方法
浓度 处理时间
K562S and K562R cells
MTT assay K562S and K562R cells were cultured in a 96-well plate (SPL) at a density of 1 × 104 cells in 100 μL of medium per well and treated with the indicated concentration of Imatinib or the AGM130 compound for 72 h. To measure the cell viability, the EZ-Cytox Cell Viability Assay kit was used. Ten microliters of MTT reagent was evenly treated in each well and incubated at 37 ◦C and 5% CO2 for 6 h. At the end of the incubation, the MTT factors of incubated cells in the plate were measured at the 450 nm wavelength using an ELISA detector.
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Idarubicin 目录号M2001
化学数据 分子量 分子式 CAS号 储存条件
497.49 C26H27NO9 58957-92-9 3年 -20°C 粉末状
溶解性(25°C)
DMSO Water <1 mg/mL Ethanol <1 mg/mL
Daunorubicin versus mitoxantrone versus idarubicin as induction and consolidation chemotherapy for adults with acute myeloid leukemia: the EORTC and GIMEMA Groups Study AML-10. Mandelli F, et al. J Clin Oncol. 2009 Nov 10;27(32):5397-403. PMID: 19826132.
Phase 2 randomized study of p53 antisense oligonucleotide (cenersen) plus idarubicin with or without cytarabine in refractory and relapsed acute myeloid leukemia. Cortes J, et al. Cancer. 2012 Jan 15;118(2):418-27. PMID: 21717444.
0~10 μM
72 h
动物实验 动物模型 配制 剂量 给药处理
Imatinibresistant K562 cells xenograft model using BALB/c nude mice saline 15 mg/kg i.p.
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
Stereoselectivity of idarubicin reduction in various animal species and humans. Strolin Benedetti M, et al. Xenobiotica. 1991 Apr;21(4):473-80. PMID: 1897247.
Prognostic significance of alterations in IDH enzyme isoforms in patients with AML treated with high-dose cytarabine and idarubicin. Ravandi F, et al. Cancer. 2012 May 15;118(10):2665-73. PMID: 22020636.
小鼠
大鼠

豚鼠
仓鼠

重量 (kg)
0.02
0.15
1.8
0.4
0.08
10
体表面积 (m2)
0.007
0.025
0.15
0.05
0.02
0.5
Km 系数
3
6
12
8
5
20
动物 B的Km系数 动物 A (mg/kg) = 动物 B (mg/kg) ×
动物 A的Km系数
例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),
得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
参考文献 5'-OH-5-nitro-Indirubin oxime (AGM130), an Indirubin derivative, induces apoptosis of Imatinib-resistant chronic myeloid leukemia cells. Kim WS, et al. Leuk Res. 2013 Apr;37(4):427-33. PMID: 23337400.
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