EGFR-IN-165 is a potent EGFR inhibitor with IC50 values of 17.18 nM for EGFRL858R/T790M kinase and 64.74 nM for EGFRWT. Its IC50 values for NCI-H1975 and A431 cell lines are 2.17 μM and 6.2 μM, respectively. EGFR-IN-165 significantly inhibits cell migration, induces G1 phase cell cycle arrest, and causes apoptosis. It is suitable for research on cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

EGFR-IN-165 (Compound 4b) effectively inhibits EGFR phosphorylation in A431 and NCI-H1975 cells in a concentration-dependent manner when applied at 0-5 μM for 48 hours. At 10 μM for 24 hours, it successfully inhibits the migration of A431 cells. At a concentration of 20 μM for 48 hours, it induces an apoptosis rate of 12.91% in NCI-H1975 cells. Additionally, EGFR-IN-165 causes G1 phase cell cycle arrest in NCI-H1975 cells when used at 2.5-20 μM for 24-48 hours. The compound exhibits extremely high stability in human plasma with a half-life of 38.5 hours and very low clearance in liver microsomes, with an intrinsic clearance rate of 24.3 mL/min/kg.