EGFR-IN-11

EGFR-IN-11 is a fourth-generation EGFR -tyrosine kinase inhibitor ( EGFR-TKI ) with an IC 50 of 18 nM for triple mutant EGFR L858R/T790M/C797S . EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis , and arrest cell cycle at G0/G1 In Vitro EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC 50 s of 0.88 nM and 0.20 µM, respectively. 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. EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Human lung cancer cell lines HCC827 (EGFR Del E746-A750 ), H1975 (EGFR L858R/T790M ) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT) Concentration: 0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 µM Incubation Time: 72 hours Result: Inhibited HCC827 H1975 A549 cells proliferation with IC 50 s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively. Western Blot AnalysisCell Line: HCC827, H1975 and A549 cells Concentration: 1.00, 0.10 and 0.01 µM for HCC827 cells; 10.00, 1.00 and 0.10 µM for H1975 and A549 cells Incubation Time: 8 hours Result: Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines. Apoptosis AnalysisCell Line: HCC827 cells Concentration: 1 µM Incubation Time: 24 hours Result: The percentages of apoptotic cells is 56.91%. Cell Cycle AnalysisCell Line: HCC827 cells Concentration: 1 µM Incubation Time: 24 hours Result: The number of HCC827 cells in G0/G1 phase was increased significantly. Form:Solid IC50& Target:EGFR L858R/T790M/C797S 18 nM (IC 50 )

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