BM-1197 (BM1197) is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL with Ki of < 1 nM, >1,000-fold selectivity over Mcl-1.
BM-1197 induces mechanism-based apoptosis in Mcl1-deficient mouse embryonic fibroblast (MEF) cells.
BM-1197 disrupts the association between BCL-XL and PUMA, induces BAX translocation and cytochrome c release and BAX/BAK-dependent apoptosis in MEF/MCL1 −/− cells.
BM-1197 exerts potent growth-inhibitory activity against small cell lung cancer (SCLC) cells in vitro (H146, IC50=3 nM).
BM-1197 IV daily at 10 mg/kg (5 days per week for 2 weeks) exhibited antitumor efficacy in SCID mice bearing H146 or H1963 cells.
