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2068806-31-3

2068806-31-3 structure
2068806-31-3 structure
  • Name: JBJ-03-142-02
  • Chemical Name: EGFR-HER2 Ex20Ins inhibitor 1a
  • CAS Number: 2068806-31-3
  • Molecular Formula: C25H22FN7O3
  • Molecular Weight: 487.495
  • Create Date: 2020-01-20 19:18:56
  • Modify Date: 2024-06-10 15:36:19
  • EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP); exhibits superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations (IC50=7.5-35 nM), and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127 compared with afatini; induces a dose-dependent reduction of EGFR and Erk phosphorylation in EGFR InsSVD transformed Ba/F3 cells with strong inhibition at 0.1 uM; displays broad and superiorantiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.

Name EGFR-HER2 Ex20Ins inhibitor 1a
Description EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP); exhibits superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations (IC50=7.5-35 nM), and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127 compared with afatini; induces a dose-dependent reduction of EGFR and Erk phosphorylation in EGFR InsSVD transformed Ba/F3 cells with strong inhibition at 0.1 uM; displays broad and superiorantiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.
References References 1. Jang J, et al. Angew Chem Int Ed Engl. 2018 Jul 6. doi: 10.1002/anie.201805187. View Related Products by Target EGFR
Molecular Formula C25H22FN7O3
Molecular Weight 487.495