EGFR-IN-8 (C09-1130-730)

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 NSCLCIn VitroEGFR-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 VivoEGFR-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.Form:SolidIC50& Target:EGFR,c-Met. Specifications and Purity: 98%. Molecular Formula: C32H23ClF3N7O4. Molecular Weight: 662.02. PubChem CID: 139035057. Isomeric SMILES: C1CC1C(=O)NC2=C(C=C(C=C2)NC(=O)NC3=CC=CC(=C3)C4=NC(=NO4)C5=C(C=C(C=C5)NC(=O)C6=CN=CC=C6)Cl)C(F)(F)F.