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BM-1197

Catalog No. T38810 CAS 1391107-89-3

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.

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BM-1197, CAS 1391107-89-3

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	BCL-XL:5.2 nM (IC50), BCL2:3.5 nM (IC50)
In vitro	BM-1197, at concentrations ranging from 2-2000 nM over 3 days, demonstrates limited cytotoxicity against wild-type mouse embryonic fibroblast (MEF) cells but significantly inhibits the growth of MCL1 Δ/Δ cells[1]. In small cell lung cancer (SCLC) lines, BM-1197 shows potent growth-inhibitory effects in 7 cell lines with IC50s below 100 nM, moderate effects in 3 cell lines with IC50s around 600 nM, and weak effects in 2 cell lines with IC50s above 2000 nM[1]. At a concentration of 100 nM for 16 hours, BM-1197 strongly induces apoptosis in H146 cells[1]. Furthermore, within 2 hours at the same concentration, it disrupts the interaction between Bcl-xl and either Puma or Bim in H146 cells[1]. BM-1197 also prompts Bax translocation within 0.5 to 2 hours and cytochrome c release within 2 hours at concentrations ranging from 3-30 nM in H146 cells[1]. Various assays confirmed these activities: a Cell Proliferation Assay showed inhibition of MCL1 Δ/Δ cell proliferation at 2-2000 nM over 3 days; an Apoptosis Analysis indicated BM-1197 induced apoptosis in H146 cells at 100 nM over 16 hours in a Bax/Bak-dependent manner; and Western Blot Analysis revealed that at 100 nM over 2 hours, BM-1197 attenuated associations between Bcl-xL and BimEL or Puma in H146 cells[1].
In vivo	BM-1197, administered intravenously (i.v.) at a dose of 10 mg/kg daily for five days per week over two weeks, elicited rapid and complete tumor regression in mice models for both H146 and H1963 tumors, with all eight mice showing no signs of the tumor[1]. At a higher dosage of 15 mg/kg, BM-1197 induced reversible thrombocytopenia, displaying its safety at efficacious levels[1]. Furthermore, this compound demonstrated notable anti-tumor effects and tolerability in OCI-Ly8 xenograft models when given at 10 mg/kg i.v. once daily (qd)[2]. In an animal model using SCID mice implanted with H146 cells, the treatment regimen resulted in the mice remaining tumor-free for at least 32 days post-therapy[1].

Molecular Weight	1131.77
Formula	C53H59ClF4N6O7S4
CAS No.	1391107-89-3

Storage

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

References and Literature

1. Bai L, et, al. BM-1197: a novel and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo. PLoS One. 2014 Jun 5; 9(6): e99404. 2. Sun YL, et, al. A novel Bcl-2 inhibitor, BM-1197, induces apoptosis in malignant lymphoma cells through the endogenous apoptotic pathway. BMC Cancer. 2019 Dec 31; 20(1):1.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BM-1197 1391107-89-3 BM 1197 BM1197 inhibitor inhibit

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