BM-1074

BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with K_i values of < 1 nM and IC₅₀ values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC₅₀ values of 1-2 nM^[1]. IC50 & Target: IC₅₀: 1.8 nM (Bcl-2), 6.9 nM (Bcl-xL)^[1] In Vitro: BM-1074 (Compound 32) shows high binding affinity to both Bcl-2 and Bcl-xL proteins and exhibits inhibitory activity against H146, H1963, H187, and H1417 cell lines^[1]. In Vivo: BM-1074 (i.v., 15 mg/kg, daily, 5 days a week for 2 weeks) exhibits the maximum tolerated dose (MTD) (15 mg/kg) and strong antitumor activity in H146 tumor xenograft mice, as well as shows no significant weight loss (<5%) or other signs of toxicity^[1].
BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues^[1].