CAS:1228108-65-3Sabutoclax

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Synonyms: BI-97C1

Sabutoclax is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1228108-65-3

储存条件

分子式

C42H40N2O8

运输

蓝冰

分子量

700.78

别名

BI-97C1

溶解度

动物实验配方

生物活性

描述Sabutoclax is a novel and effective pan-Bcl-2 antagonist with IC50 values of 0.31, 0.32, 0.20, and 0.62μM for inhibiting the binding of BH3 peptides to Bcl-XL, Bcl-2, Mcl-1, and Bfl-1. It potently inhibited cell growth of human prostate cancer PC-3, lung cancer H460, and lymphoma cell BP3 with EC50 values of 0.13, 0.56, and 0.049μM, respectively. Consistent with this in vitro study, Sabutoclax displayed antitumor efficacy in vivo as administration of Sabutoclax at 5mg/kg, i.p., every 2 days (total of nine injections), suppressed tumor growth of prostate cancer M2182 xenograft mouse model. Sabutoclax at 1μM significantly increased the apoptosis of BC LSCs measured by cleaved capase-3 and PI staining in vitro and sensitized marrow niche-engrafted BC LSCs to Dasatinib in vivo at 5mg/kg.