A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.
IC50&Target
Mcl-1
0.45 nM (Ki)
Bcl-2
132 nM (Ki)
Bfl-1
660 nM (Ki)
Bcl-W
2280 nM (Ki)
Apoptosis
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.
分子式
C46H55N7O7S
分子量
850.04
CAS号
1668553-26-1
运输条件
Room temperature in continental US; may vary elsewhere.