Description
SU-4312 (5812-07-7) is a potent selective inhibitor of VEGFR kinase (also known as Flk-1 and KDR). Inhibition of the activated kinase (IC50 = 0.4 μM) is 100-fold less than inhibition of the unactivated kinase (IC50 = 0.04 μM). SU-4312 also inhibits PDGFR kinase (IC50 = 19.4 μM).
Uses
SU 4312 is a vascular endothelial growth factor receptor KDR tyrosine kinase antagonist.
Definition
ChEBI: A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group. SU 4312 is a vascular endothelial growth factor (VEGF) receptor protein
yrosine kinase 1/2 and platelet derived growth factor (PDGF) receptor inhibitor. It also inhibits the neuronal nitric oxide synthase (NOS) and exhibits neuroprotection against NO-mediated neurotoxicity.
Biological Activity
Potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC 50 values are 0.8 and 19.4 mM respectively). Selective over EGFR and c-Src tyrosine kinases.
References
[1] R L KENDALL. Vascular endothelial growth factor receptor KDR tyrosine kinase activity is increased by autophosphorylation of two activation loop tyrosine residues.[J]. The Journal of Biological Chemistry, 1999, 274 10: 6453-6460. DOI:
10.1074/jbc.274.10.6453[2] LI SUN. Synthesis and Biological Evaluations of 3-Substituted Indolin-2-ones: A Novel Class of Tyrosine Kinase Inhibitors That Exhibit Selectivity toward Particular Receptor Tyrosine Kinases[J]. Journal of Medicinal Chemistry, 1998, 41 14: 2588-2603. DOI:
10.1021/jm980123i
