Sunitinib (SU11248) is a multi-targeted RTK inhibitor that targets VEGFR2 (Flk-1) and PDGFRβ with Ki of 8 nM and 9 nM respectively.
Sunitinib displays >10-fold higher selectivity over FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and Src.
Sunitinib also inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM.
Sunitinib regresses FLT3-ITD tumors in the subcutaneous tumor xenograft model.
