A-1210477
$100.00 – $395.00
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| Catalog No. | APIM050276 |
|---|---|
| Product Name | A-1210477 |
Description
Background Information:
A-1210477 is a proteolytically stable, cell-permeable and high affinity BH3 mimetics 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).
Reference:
1. D 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.
APIM050276: A-1210477
CAS No.: 1668553-26-1.
Molecular Formula: C46H55N7O7S ? 0.5xHCl.
Molecular Weight: 868.3.
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
