ARN25062 is a derivative of ARN22089, an inhibitor of the protein-protein interaction between Cdc42 and p21-activated kinase (PAK).[1] It inhibits the proliferation of SKM28, SK-MEL-3, WM3248, and A375 melanoma cells (IC50s = 6.1, 4.6, 9.3, and 5.1 µM, respectively) and SW480 colon cancer cells (IC50 = 5.9 µM). ARN25062 (10 mg/kg) reduces tumor growth in a patient-derived xenograft (PDX) mouse model.
References:
[1].Brindani, N., Vuong, L.M., Acquistapace, I.M., et al.Design, synthesis, in vitro and in vivo characterization of CDC42 GTPase interaction inhibitors for the treatment of cancerJ. Med. Chem.66(8)5981-6001(2023).