ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects[1].
ATH686 (1-100 µM; 3 days) potently inhibits cell proliferation (IC50 around 0.001 µM) via induction of apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells[1]. ATH686 (10 nM; for 15 minutes) inhibits autophosphorylation of mutant FLT3 in FLT3-ITD-Ba/F3 cells[1].
[1]. Ellen Weisberg, et al. Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison. Genes Cancer. 2010 Oct;1(10):1021-32.