EGFR-IN-11 |
| Katalog-Nr.GC62562 |
EGFR-IN-11 ist ein EGFR-Tyrosinkinase-Inhibitor (EGFR-TKI) der vierten Generation mit einem IC50 von 18 nM fÜr die Dreifachmutante EGFRL858R/T790M/C797S. EGFR-IN-11 unterdrÜckt signifikant die EGFR-Phosphorylierung, induziert die Apoptose und hÄlt den Zellzyklus bei G0/G1 an.
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Cas No.: 2463200-44-2
Sample solution is provided at 25 µL, 10mM.
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EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1].
EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 µM, respectively[1]. EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1]. EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.[1]EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell[1].
[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.
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