EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC
In Vitro
EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC 50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively. EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549, PC9, H1975, CL68, and CL97 cells Concentration: 0-20 μM Incubation Time: 24 hours, 48 hours, 72 hours Result: Showed inhibitory effects on different cells. Western Blot AnalysisCell Line: A549, PC9, H1975, CL68, and CL97 cells Concentration: 0-0.6 μM Incubation Time: 48 hours Result: Decreased EGFR and c-Met expression.
In Vivo
EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice H1975 xenograft tumor model Dosage: 50 and 150 mg/kg Administration: Oral gavage; 50 and 150 mg/kg; once daily; 20 days Result: Inhibited H1975 xenograft tumor growth.
IC50& Target:EGFR,c-Met
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