Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z, Sheets M, St Martin T, Karp R, van Kalken D, Chaturvedi P, Niu D, Nacht M, Petter RC, Westlin W, Lin K, Jaw-Tsai S, Raponi M, Van Dyke T, Etter J, Weaver Z, Pao W, Singh J, Simmons AD, Harding TC, Allen A
Cancer Discov. 2013 3 (12): 1404-15

PMID: 24065731 · PMCID: PMC4048995 · DOI:10.1158/2159-8290.CD-13-0314

MeSH Terms (24)

Acrylamides Administration, Oral Animals Antineoplastic Agents Carcinoma, Non-Small-Cell Lung Cell Line, Tumor Cell Proliferation Drug Resistance, Neoplasm Drug Screening Assays, Antitumor Epithelial-Mesenchymal Transition ErbB Receptors Female HEK293 Cells Humans Lung Neoplasms Mice Mice, Inbred BALB C Mice, Nude Mice, Transgenic Molecular Targeted Therapy Mutant Proteins Protein Kinase Inhibitors Pyrimidines Xenograft Model Antitumor Assays

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