Sunitinib . malate

Potent ATP-competitive and cell permeable multi-targeted receptor tyrosine kinase (RTK) inhibitor targeting VEGFR and PDGFR-beta. Inhibits FLK1 (Ki=9nM), PDGFRbeta (Ki=8nM) and FLT3. It is at least 10-fold selective for FLK1 and PDGFRbeta over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl and Src. Inhibits the cellular receptor phosphorylation of FLT3, RET and CSF-1R. Also shown to inhibit c-Kit. Exhibits potent antiangiogenic and antitumor activity in multiple xenograft models.