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AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
Cancer Cell · 2009 · Vol. 16(5) · pp. 401–412
Thomas O’Hare✉(Howard Hughes Medical Institute)William C. Shakespeare(Ariadne Diagnostics (United States))Xiaotian Zhu(Ariadne Diagnostics (United States))Christopher A. Eide(Oregon Health & Science University)Victor M. Rivera(Ariadne Diagnostics (United States))Frank Wang(Ariadne Diagnostics (United States))Lauren T. Adrian(Oregon Health & Science University)Tianjun Zhou(Ariadne Diagnostics (United States))Wei-Sheng Huang(Ariadne Diagnostics (United States))Qihong Xu(Ariadne Diagnostics (United States))Chester A. Metcalf(Ariadne Diagnostics (United States))Jeffrey Tyner(Oregon Health & Science University)Marc Loriaux(Oregon Health & Science University)Amie S. Corbin(Oregon Health & Science University)Scott Wardwell(Ariadne Diagnostics (United States))Yaoyu Ning(Ariadne Diagnostics (United States))Jeffrey Keats(Ariadne Diagnostics (United States))Yihan Wang(Ariadne Diagnostics (United States))Raji Sundaramoorthi(Ariadne Diagnostics (United States))Mathew Thomas(Ariadne Diagnostics (United States))Dong Zhou(Ariadne Diagnostics (United States))J. T. Snodgrass(Ariadne Diagnostics (United States))Lois Commodore(Ariadne Diagnostics (United States))Tomi K. Sawyer(Ariadne Diagnostics (United States))David C. Dalgarno(Ariadne Diagnostics (United States))Michael W. Deininger(Oregon Health & Science University)Brian Druker(Oregon Health & Science University)Tim Clackson(Ariadne Diagnostics (United States))
Chronic Myeloid Leukemia TreatmentsChronic Lymphocytic Leukemia ResearchEosinophilic Disorders and SyndromesMyeloid leukemiaMutantMutationCancer researchABLbreakpoint cluster regionMyeloidBiologySignal transductionGene
MeSH terms
AnimalsAntineoplastic AgentsHumansImidazolesModels, MolecularPyridazinesSignal TransductionLeukemia, Myelogenous, Chronic, BCR-ABL PositiveFusion Proteins, bcr-ablProto-Oncogene Proteins c-ablMice, SCIDCrystallography, X-RayCell Line, TumorProtein Kinase InhibitorsCell Growth Processes
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References
Discovery of <i>N</i>-(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays
Journal of Medicinal Chemistry · 2004 · 1,285 citations
A quantitative analysis of kinase inhibitor selectivity
Nature Biotechnology · 2008 · 2,427 citations
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
Cancer Cell · 2005 · 1,480 citations
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