| 產(chǎn)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 |
| 靶點(diǎn)： |
Mcl-1:0.45 nM (Ki);Bcl-2:132 nM (Ki);Bfl-1:660 nM (Ki);Bcl-W:2280 nM (Ki);Apoptosis;Apoptosis;BCL |
| 體外研究： |
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 |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。 |
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