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A-1331852
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.
Catalog NO: CT-A133
Synonym: A1331852
CAS NO: 1430844-80-6
Mol. Formula: C38H38N6O3S
MW: 658.8 (or refer to the Certificate of Analysis, batch-specific)
** in vivo grade material, >99.5% pure, white powder, clean (See All QC Docs Attached), Hemihydrate, HCl free, validated by a spot-on Quantitative Microanalysis. Bulk Stock! Same day shipping.