Discovery of clinical candidate BMS-906024: A potent pan-notch inhibitor for the treatment of leukemia and solid tumors

ACS Medicinal Chemistry Letters

Volumn 6, Issue 5, 2015, Pages 523-527

  Gavai, Ashvinikumar V ^a   Quesnelle, Claude ^a   Norris, Derek ^a   Han, Wen Ching ^a   Gill, Patrice ^a   Shan, Weifang ^a   Balog, Aaron ^a   Chen, Ke ^c   Tebben, Andrew ^a   Rampulla, Richard ^a   Wu, Dauh Rurng ^a   Zhang, Yingru ^a   Mathur, Arvind ^a   White, Ronald ^a   Rose, Anne ^a   Wang, Haiqing ^a   Yang, Zheng ^a   Ranasinghe, Asoka ^a   D'Arienzo, Celia ^a   Guarino, Victor ^a   Xiao, Lan ^a   Su, Ching ^a   Everlof, Gerry ^a   Arora, Vinod ^b   Shen, Ding Ren ^a   Cvijic, Mary Ellen ^a   Menard, Krista ^a   Wen, Mei Li ^a   Meredith, Jere ^b   Trainor, George ^a   Lombardo, Louis J ^a   Olson, Richard ^b   Baran, Phil S ^c   Hunt, John T ^a   Vite, Gregory D ^a   Fischer, Bruce S ^a   Westhouse, Richard A ^a   Lee, Francis Y ^a   more..

^a BRISTOL MYERS SQUIBB RESEARCH AND DEVELOPMENT   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

^c SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

Notch inhibitor; SAR; T acute lymphoblastic leukemia; triple negative breast cancer; secretase inhibitor

Indexed keywords

ANTILEUKEMIC AGENT; ANTINEOPLASTIC AGENT; BMS 906024; GAMMA SECRETASE INHIBITOR; NOTCH RECEPTOR; NOTCH1 RECEPTOR; NOTCH2 RECEPTOR; NOTCH3 RECEPTOR; NOTCH4 RECEPTOR; UNCLASSIFIED DRUG;

ACUTE LYMPHOBLASTIC LEUKEMIA; AEROBIC METABOLISM; ALKYLATION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL PROLIFERATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG PENETRATION; EPIMERIZATION; GENE MUTATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; METABOLIC STABILITY; MOUSE; NONHUMAN; OXIDATION; PLASMA HALF LIFE; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; SOLID TUMOR; STRUCTURE ACTIVITY RELATION; T CELL LEUKEMIA; TIME TO MAXIMUM PLASMA CONCENTRATION; TRIPLE NEGATIVE BREAST CANCER; TUMOR XENOGRAFT;

EID: 84929331637     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00001     Document Type: Article

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