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KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase with IC50 values of 6.6nM, 14nM, 4nM and 48nM, respectively [1].

KW-2449 is a potent kinase inhibitor against FLT3, ABL, T315I-mutant ABL (ABL-T315I) tyrosine kinases as well as Aurora kinase. In vitro assay shows KW-2449 has the potency of growth inhibition with different mechanisms. In leukemia cells with FLT3 mutations, KW-2449 down-regulates phosphorylated-FLT3/STAT5, induces G1 arrest and apoptosis. KW-2449 also inhibits tumor growth in FLT3-mutated xenograft model. While in leukemia cells with wild-type FLT3, KW-2449 reduces phosphorylated histone H3, induces G2/M arrest and apoptosis. However, it is reported that the AML patients treated with LT3 inhibitors, such as KW-2449, have only partial FLT3 inhibition in vivo. And the plasma level of FL (the ligand of FLT3) appears to rise after chemotherapy, which impeding the efficacy of the FLT3 inhibitors [1, 2].

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