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BM-1074
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。
BM-1074图片
CAS NO:1391108-10-3
规格:98%
分子量:1013.68
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Bcl-2/Bcl-xL inhibitor,potent and selective
CAS:1391108-10-3
分子式:C50H57ClN8O7S3
分子量:1013.68
纯度:98%
存储:Store at -20°C

Background:

BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].


BM-1074 is a selective Bcl-2 and Bcl-xL inhibitor. It shows high binding affinity to both Bcl-2 and Bcl-xL. In H146 cell line, BM-1074 inhibits the cell growth with IC50 value of 1.3nM. It is found that 15 mg/kg dosed intravenously is the maximum tolerated dose (MTD) of BM-1074. BM-1074 at MTD induces cleavage of PARP and caspase-3 in H146 xenograft tumors in SCID mice, indicating a strong apoptosis induction in vivo. BM-1074 also shows rapid, complete and persistent antitumor efficacy in the H-146 xenograft model. Moreover, mice treated with BM-1074 shows no significant weight loss or other toxicity signs. In addition, BM-1074 inhibits cell growth in three other small-cell lung cancer cell lines, including H1963, H187 and H1417, with IC50 values of 1nM, 1.4nM and 2.3nM, respectively [1].


参考文献:
[1] Aguilar A, Zhou H, Chen J, Liu L, Bai L, McEachern D, Yang CY, Meagher J, Stuckey J, Wang S. A potent and highly efficacious Bcl-2/Bcl-xL inhibitor. J Med Chem. 2013 Apr 11;56(7):3048-67.