Description
As a multi-target inhibitor, KW-2449 potently inhibits Flt3, Abl and Aurora A with IC50 of 6.6 nM, 14 nM and 48 nM.
In vitro
As a multi-target inhibitor, KW-2449 potently inhibits Flt3, Abl and Aurora A with IC50 of 6.6 nM, 14 nM and 48 nM, respectively. KW-2449 showed the potent growth inhibitory effects on leukemia cells with FLT3 mutations by inhibition of the FLT3 kinase, resulting in the down-regulation of hosphorylated-FLT3/STAT5, G(1) arrest, and apoptosis. In FLT3 wild-type human leukemia, it induced the reduction of phosphorylated histone H3, G(2)/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributed to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases.
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