FAK-IN-28 is an orally active FAK inhibitor with an IC50 of 0.4 nM. It exhibits both antiproliferative and antimetastatic effects. FAK-IN-28 induces apoptosis by triggering caspase-3-dependent pathways through increased ROS levels. This compound effectively inhibits tumor growth without causing weight loss or hepatorenal toxicity. FAK-IN-28 is suitable for research on FAK-driven malignancies, including colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.

FAK-IN-28 (Compound 10c) exhibits cytotoxic effects on HCT116, HeLa, MDA-MB-231, and A375 cells, with IC50 values of 0.08, 0.31, 0.23, and 0.29 μM, respectively, over 12 hours. It inhibits HCT116 cell invasion and reduces the number of adherent cells at concentrations of 0.2-25 μM for 1-24 hours. Additionally, FAK-IN-28, at 0.2-25 μM for 12-24 hours, enhances caspase-3 activation, increases apoptotic cell count, and disrupts the cell cycle progression in HCT116 cells. Furthermore, at 1-125 μM over 12 hours, FAK-IN-28 induces ROS activity in HCT116 cells.

FAK-IN-28 (Compound 10c) administered orally at a dose of 50 mg/kg once daily for 10 days effectively inhibits tumor growth in an HCT116 xenograft nude mouse model, while not causing significant weight loss or inducing hepatotoxicity or nephrotoxicity.