BM-1074

BM-1074 是一种有效且特异性的 Bcl-2/Bcl-xL 抑制剂，对 Bcl-2 和 Bcl-xL 的 Ki 值 < 1 nM，IC50 值分别为 1.8 nM 和 6.9 nM。 BM-1074 诱导细胞凋亡，并对四种小细胞肺癌细胞系（H146、H1963、H187 和 H1417）具有抗增殖活性，IC50 值为 1-2 nM。

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库存: 现货

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10mg

￥1425.00

1140.00

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25mg

￥2950.00

2360.00

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50mg

￥4962.00

3970.00

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100mg

￥8900.00

7120.00

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货号: ajci11238
CAS: 1391108-10-3
别名:
分子式: C50H57ClN8O7S3
分子量: 1013.68
纯度: >98%
溶解度: DMSO mg/mL Water mg/mL Ethanol mg/mL
储存: Store at -20°C
库存: 现货

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.