EGFR-IN-46

EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

EGFR:20.17 nM (IC50)

FAK:14.25 nM (IC50)

EGFR-IN-46 (compound 6h) (0-100 µM; 24 h) inhibits the growth activity against DLD1, HCT-116 cells with IC50s of 1.79, 3.28 µM, respectively[1]. EGFR-IN-46 (3 µM; 24 h) induces cell apoptosis in DLD1 cells[1]. EGFR-IN-46 exhibits weak TOP1 (Topoisomerase I) poisoning effect (-/+)[1]. Cell Proliferation Assay[1] Cell Line: DLD1, HCT-116, MDMBA-231, MCF-7, Hela cells Concentration: 10 µM Incubation Time: 24 h Result: Showed excellent growth inhibition with the percent growth inhibition of 92.36%, 89.34%, 84.76%, 90.36%, 90.78% for DLD1, HCT-116, MDMBA-231, MCF-7, Hela cells, respectively. Apoptosis Analysis[1] Cell Line: DLD1 cells Concentration: 3 µM Incubation Time: 24 h Result: Increased the total percentage of apoptotic cells from 7% to 90.33%.

[1]. Elbadawi MM, et al. 2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights. J Enzyme Inhib Med Chem. 2022 Dec;37(1):349-372.