上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
BM-1197
BM-1197 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。
BM-1197 Chemical Structure
CAS No. : 1391107-89-3
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
BM-1197 is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo[1][2].
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| IC50 & Target[1] |
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Bcl-2
3.5 nM (IC50)
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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 the MCL1−/− 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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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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