Chemical Name: (4-Fluorophenyl)methyl N-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-N-[3-[(1-oxo-2-propen-1-yl)amino]phenyl]carbamate
Biological ActivityJBJ-03-142-02 is a highly potent epidermal growth factor receptor (EGFR) and ErbB2 (human epidermal growth factor receptor; HER2) inhibitor. Inhibits wild type and tumorgenic mutated receptors (exon 20 insertion; Ex20Ins). Antiproliferative in vitro (IC50 values are 7.6, 30 - 95, 3.8 and 19 - 31 nM for Ba/F3 cells expressing wild type EGFR, EGFR with Ex20Ins mutation, wild type HER2 and HER2 with Ex20Ins mutation, respectively). Also inhibits other common EGFR mutants. Antiproliferative in patient-derived lung cancer cell lines.
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Discovery of a highly potent and broadly effective epidermal growth factor receptor and HER2 exon 20 insertion mutant inhibitor.
Jang et al.
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