Sunitinib malate (341031-54-7) is a potent inhibitor of multiple receptor tyrosine kinases including VEGFR, PDGFRβ and Kit (Ki = 2-17 nM)1. Also inhibits cFMS (IC50=7 nM)2 and FLT33. Potent inhibitor of angiogenesis.4 Sunitinib malate is a clinically useful anticancer agent. Cell permeable.
1) Deeks et al. (2006), Sunitinib; Drugs, 66 2255
2) Guo et al. (2006), Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors; Mol. Cancer. Ther., 5 1007
3) O’Farrell et al. (2003), SU11248 is a novel FLT3 yrosine kinase with potent activity in vitro and in vivo; Blood, 101 3597
4) Roskoski et al. (2007), Sunitinib: a EGF and PDGF receptor protein kinase and angiogenesis inhibitor; Biochem. Biophys. Res. Commun., 356 323