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BM-1197

产品编号 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

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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.
靶点活性	BCL-XL:5.2 nM (IC50), BCL2:3.5 nM (IC50)
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.

分子量	1131.77
分子式	C53H59ClF4N6O7S4
CAS No.	1391107-89-3

存储

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

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参考文献

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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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