(E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-[(3-phenyl-n-propyl)amino-carbonyl]acrylonitrile Pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent and selective inhibitor of Flk-1 kinase (IC50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Also reduces the expression of ets-1, a transcription factor stimulated by VEGF. Has only a weak inhibitory effect on PDGF-receptor (IC50 >50 µM), EGF-receptor (IC50 >100 µM), and HER2 (IC50 >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay. Purity: ≥95% by HPLC. Ref.: Arbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469. Strawn, L.M., et al. 1996. Cancer Res. 56, 3540. |
