FAK-IN-33

FAK-IN-33 (compound 5f) (0.005-50 μM; 72 h) potently inhibits the proliferation of U118-MG glioblastoma cells, with an IC₅₀ of 0.29 μM^[1].
FAK-IN-33 (72 h) exhibits low toxicity to LO2 normal hepatocytes (IC₅₀ = 7.12 μM) and 2BS normal fibroblasts (IC₅₀ = 32.10 μM), demonstrating selective activity against tumor cells^[1].
FAK-IN-33 potently inhibits purified FAK kinase with an IC₅₀ of 10.23 nM^[1].
FAK-IN-33 exhibits stronger binding affinity to FAK kinase (PDB ID: 2JKK) than TAE-226, forms an additional hydrogen bond with Glu502, and has a shorter binding distance^[1].
FAK-IN-33 (0.04-2 μM) induces apoptosis in U118-MG cells in a concentration-dependent manner; at 2 μM, the proportion of late apoptotic cells increases from 2.54% in the control group to 16.5%, and the proportion of total apoptotic cells is approximately twice that of the TAE-226 group at the same concentration^[1].
FAK-IN-33 (0.2-0.8 μM; 24 h) induces G2/M phase arrest in U118-MG cells; the proportion of cells in G2/M phase increases from 7.84% in the control group to 68.61% at 0.2 μM and 78.09% at 0.8 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.