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Discovery of a Potent and Selective BCL-XL Inhibitor With in Vivo Activity

Discovery of a Potent and Selective BCL-XL Inhibitor With in Vivo Activity

Zhi-Fu Tao, Lisa Hasvold, Le Wang, Xilu Wang, Andrew M Petros, Chang H Park, Erwin R Boghaert, Nathaniel D Catron, Jun Chen, Peter M Colman, Peter E Czabotar, Kurt Deshayes, Wayne J Fairbrother, John A Flygare, etc.

ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.

PMID: 25313317

Abstract:

A-1155463, a highly potent and selective BCL-XL inhibitor, was discovered through nuclear magnetic resonance (NMR) fragment screening and structure-based design. This compound is substantially more potent against BCL-XL-dependent cell lines relative to our recently reported inhibitor, WEHI-539, while possessing none of its inherent pharmaceutical liabilities. A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses. A-1155463 thus represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
TIT9316	CombiTitrant 5 XL			Price

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