產(chǎn)品屬性：

Cas No.1391108-10-3

別名 N/A

化學(xué)名 (R,Z)-5-(4-chlorophenyl)-4-(3-(4-(4-(4-((4-(dimethylamino)-1-(phenylthio)butan-2-yl)amino)-3-nitrophenylsulfonamido)phenyl)piperazin-1-yl)phenyl)-1-isopropyl-2-methyl-N-(methylsulfonyl)-1H-pyrrole-3-carbimidic acid

分子式 C50H5

分子量 1013.68

溶解度 DMSO mg/mL Water mg/mL Ethanol mg/mL

儲(chǔ)存條件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
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].

References:

[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.