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Background Information:
A-1331852 is a 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 = 6 nM, >600-fold selectivity), BCL-W (Ki = 4 nM, >400-fold selectivity), and MCL-1 (Ki = 142 nM, >14000-fold selectivity) (ref. 1). It selectively disrupts BCL-XL–BIM complex and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50 values in the low nM range without any measurable effects on MEF cells lacking BAK or BAX (ref. 1). Orally administered A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. It significantly inhibits tumor growth given ether as a single agent, or combined with docetaxel in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer. A-1331852, together with A-1155463 (Our Prod No: CT-A115), represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity.
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. SciTransl Med. 2015 Mar 18;7(279):279ra40
APIM050002: A-1331852
CAS No.: 1430844-80-6
Molecular Formula: C38H38N6O3S.
Molecular Weight: 658.8 (or refer to the Certificate of Analysis, batch-specific).
Purity: >99.5% by HPLC at 214 and 254 nm.
QC: HPLC-MS, NMR, and Quantitative Elemental Analysis.
Solubility: DMSO.
Storage: Store at 0-4°C (short term), -20°C (Long term), Desiccated.
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