| Bioactivity | 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[2]. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| Name | A-1210477 | ||||||||||||
| CAS | 1668553-26-1 | ||||||||||||
| Formula | C46H55N7O7S | ||||||||||||
| Molar Mass | 850.04 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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