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Chemical Structure : EGFR-HER2 Ex20Ins inhibitor 1a
Catalog No.: PC-35374Not For Human Use, Lab Use Only.
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).
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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 superior antiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.
| M.Wt | 487.495 | |
| Formula | C25H22FN7O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jang J, et al. Angew Chem Int Ed Engl. 2018 Jul 6. doi: 10.1002/anie.201805187.
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