1402709-93-6

CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).

Aurora-A: 38 nM (IC₅₀); Aurora-A: 7.5 nM (Kd); Aurora-B: 48 nM (Kd); FLT3(K663Q): 5.1 nM (Kd); FLT3: 6.2 nM (Kd); FLT3(D835H): 11 nM (Kd); FLT3(D835Y): 14 nM (Kd); FLT3(N841I): 16 nM (Kd); FLT3-ITD: 38 nM (Kd); FLT3(R834Q): 110 nM (Kd)

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[1] Bavetsias V, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34. DOI:10.1021/jm300952s