FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. This compound inhibits the proliferation and colony formation of MDA-MB-231 cells and induces cell cycle arrest and apoptosis (apoptosis). FAK-IN-29 exhibits antitumor activity and is applicable for research in cancers such as triple-negative breast cancer.

FAK-IN-29 (Compound 7h) induces G2/M phase cell cycle arrest at a concentration of 3 μM over 24 hours in MDA-MB-231 cells. It has an IC50 of 0.18, 0.17, and 0.15 μM for MDA-MB-231, SKOV3, and HepG2 cells respectively, when used at 0.15625-50 μM for 48 hours. Additionally, FAK-IN-29 induces apoptosis in a concentration-dependent manner at 0.3-3 μM over 24 hours in MDA-MB-231 cells and significantly inhibits colony formation in the same cells under identical conditions.

In the MDA-MB-231 tumor xenograft model using nude mice, FAK-IN-29 (5-10 mg/kg, administered via intravenous injection over 14 days) demonstrated potent antitumor activity and exhibited favorable safety characteristics.