CAS:1260251-31-7Birinapant

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Synonyms: TL32711

Birinapant binds with XIAP and cIAP1 with K of 45 and <1 nM, respectively.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1260251-31-7

储存条件

分子式

C42H56F2N8O6

运输

蓝冰

分子量

806.94

别名

TL32711

溶解度

动物实验配方

生物活性

靶点 cIAP1

Kd:1nM XIAP

Kd:45nM
描述Birinapant binds with XIAP and cIAP1 with K of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.

靶点	Description	IC50
cIAP1		Kd:1nM
XIAP		Kd:45nM