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首页-小分子抑制剂&激动剂-Apoptosis-IAP-GDC-0152
GDC-0152

Chemical Structure : GDC-0152

CAS No.: 873652-48-3

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GDC-0152 (GDC0152)

货号: PC-25916Not For Human Use, Lab Use Only.

GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins, binds to XIAP BIR3 domain, BIR domain of ML-IAP, and BIR3 domains of cIAP1 and cIAP2 with Ki of 28, 14, 17, and 43 nM, respectively.

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5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins, binds to XIAP BIR3 domain, BIR domain of ML-IAP, and BIR3 domains of cIAP1 and cIAP2 with Ki of 28, 14, 17, and 43 nM, respectively.
GDC-0152 promotes degradation of cIAP1, induces activation of caspase-3/7, and lead to decreased viability of breast cancer cells without affecting normal mammary epithelial cells.
GDC-0152 (10-100 mg/kg) inhibits tumor growth when dosed orally in the MDA-MB-231 breast cancer xenograft model.

物理化学性质&存储条件

分子量 498.65
分子式 C25H34N6O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-1-((S)-2-Cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-N-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide

参考文献

1. Flygare JA, et al. J Med Chem. 2012 May 10;55(9):4101-13.

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