BM-1197 T38810

Product Introduction
Bioactivity


英文名: BM-1197

描述: BM-1197, a highly potent and specific dual inhibitor of Bcl-2 and Bcl-xL, effectively targets these proteins with IC50 values of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. This compound demonstrates notable antitumor activity in both in vitro and in vivo settings.

体外活性: BM-1197 (2-2000 nM; 3 d) has marginal cytotoxicity against wild-type mouse embryonic fibroblast (MEF) cells but exerts potent growth-inhibitory activity in the MCL1 ?/? cells[1]. BM-1197 shows potent growth-inhibitory activities in 7 small cell lung cancer (SCLC) cell lines with IC 50 s <100 nM, moderate activity in 3 SCLC cell lines with IC 50 s of ～600 nM and weak activity in 2 SCLC cell lines with IC 50 s >2000 nM[1]. BM-1197 (100 nM; 16 h) potently induces apoptosis in H146 cells[1]. BM-1197 (100 nM; 2 h) disrupts the association between Bcl-xl and Puma or Bim in H146 cells[1]. BM-1197 (100 nM; 0.5-2 h) induces Bax translocation, and it (3-30 nM; 2 h) induces cytochrome c release in H146 cells[1]. Cell Proliferation Assay[1]Cell Line: MEF/ MCL1 ?/? cells Concentration: 2, 20, 200, 2000 nM Incubation Time: 3 days Result: Inhibited MCL1 ?/? cells proliferation. Apoptosis Analysis[1]Cell Line: H146 cells Concentration: 100 nM Incubation Time: 16 hours Result: Induced apoptosis in a strictly Bax/Bak-dependent manner. Western Blot Analysis[1]Cell Line: H146 cells Concentration: 100 nM Incubation Time: 2 hours Result: Attenuated the associations between Bcl-xL and BimEL or Puma.

体内活性: BM-1197 (10 mg/kg; i.v. daily 5 days per week for 2 weeks) results in rapid and complete tumor regression in all 8 mice in H146 and H1963 tumor model[1]. BM-1197 (15 mg/kg; i.v.) causes thrombocytopenia in mice but the effect is reversible even at highly efficacious doses[1]. BM-1197 (10 mg/kg; i.v. qd) exerts a strong anti-tumor effect and is well tolerated in OCI-Ly8 xenograft models[2]. Animal Model: SCID mice bearing H146 cells[1]Dosage: 10 mg/kg Administration: I.v. daily 5 days per week for 2 weeks Result: Remained tumor free for at least 32 days after the end of the treatment.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: BM-1197 | BM 1197 | BM1197

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途