Description |
Sunitinib, also known as SU11248, is a multi-tyrosine kinase inhibitor widely known to target PDGFR, VEGFR, KIT, and FLT3, and therefore has both antitumor and antiangiogenic activities. Cellular phosphorylation assays show that sunitinib effectively inhibits ligand-dependent phosphorylation of these receptor tyrosine kinases in nanomolar concentrations and can also inhibit ligand-dependent cellular proliferation (1-3). Sunitinib displays greater than 10-fold selectively for PDGFRB and VEGFR over numerous other kinases, including EGFR, Cdk2, Met, IGF -1R, Abl, and src (2). Inhibition of CSF-1 (4) and RET (5) by sunitinib has also been observed.
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