Description
SU-1498 (168835-82-3) is a potent, reversible, selective inhibitor of VEGFR-2, also known as Flk-1 (IC50 = 700 nM). Inhibition of VEGFR-2 blocks angiogenesis in both in vitro and in vivo models. Cell permeable.
Uses
SU 1498 is an inhibitor of VEGF receptor kinase.
Definition
ChEBI: SU1498 is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2E)-2-cyano-3-[4-hydroxy-3,5-di(propan-2-yl)phenyl]prop-2-enoic acid with the amino group of 3-phenylpropylamine. It has a role as a vascular endothelial growth factor receptor antagonist. It is an enamide, a member of phenols, a nitrile, a monocarboxylic acid amide and a secondary carboxamide.
Biochem/physiol Actions
SU1498 is a potent and selective inhibitor of the VEGFR2 receptor kinase, Flk-1 with an IC50 value of 700 nM. SU1498 is a very weak inhibitor of PDGFR-kinase, EGFR-kinase and HER-2 kinase with IC50 values > 50 μM. SU1498 has been used to study the role of VEGFR2 (Flk-1) in a variety of biological activities including angiogenesis, tumor growth inhibition, and stem cell proliferation.
IC 50
Flk-1: 700 nM (IC50)
References
1) Cho et al. (2005), Retinoic acid and erythropoietin maintain alveolar development in mice treated with an angiogenesis inhibitor; Am. J. Respir. Cell Mol. Biol., 33 622
2) Wang et al. (2002), Interplay between integrins and FLK-1 in shear stress-induced signaling; Am. J. Physiol. Cell Physiol., 283 C1540
3) Strawn et al. (1996), FLK-1 as a target for tumor growth inhibition; Cancer Res., 56 3540
