S83365 |
CUDC-427 |
源叶(MedMol) | 99% |
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- 产品描述: CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
- 靶点: IAP
- 体外研究:
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)
- 体内研究:
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
- 参考文献:
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.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.771 ml 8.854 ml 17.709 ml 5 mM 0.354 ml 1.771 ml 3.542 ml 10 mM 0.177 ml 0.885 ml 1.771 ml 50 mM 0.035 ml 0.177 ml 0.354 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)