S80446 |
A-1210477 |
源叶(MedMol) | 98% |
- 提示:详情请下载说明书。
- 产品描述: A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM[1]. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner
- 靶点: Mcl-1:0.45 nM (Ki);Bcl-2:132 nM (Ki);Bfl-1:660 nM (Ki);Bcl-W:2280 nM (Ki);Apoptosis;Apoptosis;BCL
- 体外研究:
A-1210477 (10 μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines
- 参考文献:
1. Leverson JD, et al. Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). Cell Death Dis. 2015 Jan 15;6:e1590. 2. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.176 ml 5.882 ml 11.764 ml 5 mM 0.235 ml 1.176 ml 2.353 ml 10 mM 0.118 ml 0.588 ml 1.176 ml 50 mM 0.024 ml 0.118 ml 0.235 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)