SAR245409_934493-76-2_DataSheet_MedChemExpress
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
Product Name:
SAR245409CAS No.:
934493-76-2Cat. No.:
HY-15900Product Data Sheet
MWt:
270.29Formula:
C13H14N6O Purity :>98%
Solubility:
DMSO
Mechanisms:Biological Activity:
SAR245409(XL765)is a potent and highly selective pan
Pathways:PI3K/Akt/mTOR; Target:PI3K Pathways:PI3K/Akt/mTOR; Target:mTOR
SAR245409 (XL765) is a potent and highly selective pan inhibitor of class I PI3Ks (α/β/γ/δ, IC50=39/110/9/43 nM) with activity against mTOR(IC50=160-910
nM).
IC50 value: 9 nM (p110γ); 39/110/9/43 nM(α/β/γ/δ) [1][4]
Target: mTOR/PI3K in vitro: XL765 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ,respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM [1]. XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL765, a dual-target PI3K/mTOR inhibitor, inhibits References:
[1]. Garcia-Echeverria C, et al. Drug discovery approaches targeting the PI3K/Akt pathway in
cancer. Oncogene, 2008, 27(41), 5511-5526.[2]. Mirzoeva OK, et al. Autophagy suppression promotes apoptotic cell death in response to cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90. The effect can be recapitulated by using combinations of single-targeted compounds. XL765 significantly reduces pho...
[],p gy pp p p p p
inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma. J Mol Med, 2011, 89(9), 877-
889.[3]. Prasad G, et al. Inhibition of PI3K/mTOR pathways in glioblastoma and implications for
combination therapy with temozolomide. Neuro Oncol, 2011, 13(4), 384-392.[4]. Yu P, et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol Cancer Ther. 2014
May;13(5):1078-91.Caution: Not fully tested. For research purposes only
Medchemexpress LLC
18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S A
E m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o
m。