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CUDC-427(GDC-0917)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CUDC-427(GDC-0917)图片
CAS NO:1446182-94-0
规格:98%
分子量:564.7
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
CUDC-427是一种高效的IAP抑制剂,常用于各种癌症的治疗。
CAS:1446182-94-0
分子式:C29H36N6O4S
分子量:564.7
纯度:98%
存储:Store at -20°C

Background:

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.


GDC-0917 (0.1 nM-10 μM) induces reduction of cIAP1 levels in PBMCs in a concentration-dependent manner showing greater than 80% inhibition at concentrations greater than 0.1 µM (56.5 ng/mL)[1].


GDC-0917 (0.08-16.3 mg/kg) exhibits antitumor activity in a dose dependent manner in the MDA-MB-231-X1.1 Breast Cancer Xenograft, and GDC-0917 is well tolerated, with all dose groups experiencing a<11% decrease in mean body weight. GDC-0917 has low to moderate clearance in the mouse (12.0 mL/min/kg), rat (27.0 mL/min/kg), and dog (15.3 mL/min/kg), and high clearance in the monkey (67.6 mL/min/kg). Oral bioavailability is lowest in monkeys compared with other species[1].


[1]. Wong H, et al. Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist. Drug Metab Dispos. 2013 Dec;41(12):2104-13.