EGFR/BRAFV600E-IN-5

Description

EGFR/BRAFV600E-IN-5 Compound 7I is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 ?M and 0.037 ?M, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 ?M and 2.50 ?M against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.