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Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors

Ashvinikumar V Gavai, Claude Quesnelle, Derek Norris, Wen-Ching Han, Patrice Gill, Weifang Shan, Aaron Balog, Ke Chen, Andrew Tebben, Richard Rampulla, Dauh-Rurng Wu, Yingru Zhang, Arvind Mathur, Ronald White, etc.

ACS Med Chem Lett. 2015 Mar 11;6(5):523-7.

PMID: 26005526

Abstract:

Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses in Notch driven leukemia and solid tumor xenograft models, 12 (BMS-906024) was selected as a candidate for clinical evaluation.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1401066792 BMS-906024 BMS-906024 1401066-79-2 Price
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