A-1210477

A-1210477 is a proteolytically stable, cell-permeable and high affinity ligand of anti-apoptotic protein MCL-1, binding to the target potently and selectively with a Ki value of 0.45 nM, highly selective against closely related proteins of BCL-2 (Ki = 132 nM, >290-fold selectivity) and BCL-XL (Ki > 660 nM, >1400-fold selectivity). A-1210477 is the first-in-class small molecule MCL-1 inhibitor with sufficient potency to disrupt the tight-binding MCL-1-BIM complex in living cells, achieving the hallmarks of intrinsic apoptosis, and demonstrating clear-on-target cancer cell killing capability either as a single agent or in combination with ABT-263 (Navitoclax).

Store at 0° C (short term), -20° C (long term), desiccated

HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis

JD Leverson, et al, Potent and selective small-molecule MCL-1inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263(navitoclax), Cell Death & Disease (2015) 6, e1590; doi: 10.1038/cddis.2014.561