Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.

Li B, Wang A, Liu J, Qi Z, Liu X, Yu K, Wu H, Chen C, Hu C, Wang W, Wu J, Hu Z, Ye L, Zou F, Liu F, Wang B, Wang L, Ren T, Zhang S, Bai M, Zhang S, Liu J, Liu Q
J Med Chem. 2016 59 (18): 8456-72

PMID: 27545040 · DOI:10.1021/acs.jmedchem.6b00902

MeSH Terms (18)

Amides Animals Cell Line, Tumor Female Gastrointestinal Neoplasms Gastrointestinal Stromal Tumors Gastrointestinal Tract Halogenation Humans Methylation Mice Mice, Nude Models, Molecular Mutation Protein Kinase Inhibitors Proto-Oncogene Proteins c-kit Rats, Sprague-Dawley Structure-Activity Relationship

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