BM-1197 (UBX1967) 是一种有效的和选择性的Bcl-2/Bcl-xL的双重抑制剂，抑制 Bcl-2 和 Bcl-xL 的IC50值分别为 3.5 nM 和 5.2 nM。BM-1197 在体外和体内均表现出抗肿瘤作用。
| 生物活性 | BM-1197 (UBX1967) is a potent and selective inhibitor of dualBcl-2/Bcl-xL, withIC50s of 3.5 nM and 5.2 nM forBcl-2andBcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo[1][2]. |
| IC50& Target[1] | Bcl-2 3.5 nM (IC50) | Bcl-xL 5.2 nM (IC50) |
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体外研究
(In Vitro) | 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 theMCL1–/–cells[1].
BM-1197 shows potent growth-inhibitory activities in 7 small cell lung cancer (SCLC) cell lines with IC50s<100 nm, moderate activity in 3 sclc cell lines with ic50s of ~600 nM and weak activity in 2 SCLC cell lines with IC50s >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: | InhibitedMCL1–/–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. |
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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