SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for prostate cancer, effectively suppressing downstream effector molecules through the inhibition of SOS1 and EGFR. It induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. In prostate cancer cells PC-3, it demonstrates significant antitumor activity with an IC50 of 0.45±0.03 μM.

SOS1/EGFR-IN-1 exhibits significant inhibitory effects on PC-3 cell proliferation at concentrations of (0.5, 12.5 μM; 15 minutes), showing stronger inhibition of SOS1 and EGFR activity compared to individual SOS1 or EGFR inhibitors or their combination. When applied at (0.5, 2.5, 12.5 μM; 15 days), SOS1/EGFR-IN-1 induces apoptosis and cell cycle arrest, which effectively hinders PC-3 cell growth. It reduces RAS-GTP levels and blocks EGF-mediated pAKT level elevation in PC-3 cells at (0.5, 12.5 μM; 15 minutes). Additionally, SOS1/EGFR-IN-1 diminishes HUVEC migration into wound areas after 48 hours at concentrations (0.5, 2.5, 12.5 μM), with a significant decrease in migration index as concentration increases.

SOS1/EGFR-IN-1, when administered via intraperitoneal injection at doses of 5 and 20 mg/kg every four days for a total of six treatments, demonstrates potent induction of apoptosis, inhibition of angiogenesis and proliferation, and significant antitumor activity in vivo without notable adverse effects in a PC-3 cell-derived prostate cancer xenograft model.