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A-1155463
A-1155463
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Description
Background Information:
A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of <0.01nM (<10 pM), highly selective against closely related proteins of BCL-2 (Ki = 74nM, >7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 (Our Prod No: CT-A133), represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2–BIM, complexes, killing BCL-XL–dependent Molt-4 cells (EC50=70nM) without measurable cytotoxicity against BCL-2–dependent RS4 (ref. 1), inducing the hallmarks of intrinsic apoptosis (ref. 1).
Reference:
1. J. D. Leverson, et al, Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40.
2. ZF Tao, et al, Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity, ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.
APIM050369: A-1155463
CAS No.: 1235034-55-5.
Molecular Formula: C35H32FN5O4S2?HCl.
Molecular Weight: 760.3 (or refer to Certificate of Analysis, batch-specific).
Purity: >99.5% by HPLC at 214 and 254 nm.
QC: HPLC-MS, NMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.