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Ref Type | Journal Article | ||||||||||||
PMID | (26005526) | ||||||||||||
Authors | Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY | ||||||||||||
Title | Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors. | ||||||||||||
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Abstract Text | 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. |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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