|BM-1074 Bcl-2/Bcl-xL inhibitor,potent and selective|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||1391108-10-3||SDF||Download SDF|
|Chemical Name||(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|
|Canonical SMILES||CC(N1C(C)=C(/C(O)=N/S(C)(=O)=O)C(C2=CC(N3CCN(C4=CC=C(NS(C5=CC(N(=O)=O)=C(N[[email protected]](CSC6=CC=CC=C6)([H])CCN(C)C)C=C5)(=O)=O)C=C4)CC3)=CC=C2)=C1C7=CC=C(Cl)C=C7)C|
|Solubility||DMSO mg/mL Water mg/mL Ethanol mg/mL||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM .
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 .
 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.