EGFR/BRAFV600E-IN-5

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM 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[1].

Product Specifications

UNSPSC

12352211

Target

Apoptosis; Bcl-2 Family; EGFR; Raf

Related Pathways

Apoptosis; JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(NC1=NC=C(C2=CC=C(Cl)C=C2)S1)CN3N=NC(CSC(N4CC5=CC=CC=C5)=NC6=C(C=CC(C)=C6)C4=O)=C3

Molecular Formula

C30H24ClN7O2S2

Molecular Weight

614.14

References & Citations

[1]El-Shafey HW, et al. Design and synthesis of novel 2-S-alkylated Quinazolinones as dual BRAFV600E and EGFR inhibitors in melanoma: Mechanistic insights from apoptosis and cell cycle modulation. Bioorg Chem. 2025 Apr 28;161:108526.