2068806-31-3
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
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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 superiorantiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.
| Name | EGFR-HER2 Ex20Ins inhibitor 1a |
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| 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. |
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| 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 |