2H-Indol-2-one, 5-chloro-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-

Uses

A potent, cell-permeable, reversible, ATP-competitive, and selective inhibitor of VEGF (Flk-1; IC₅₀ = 1.2 µM) and PDGF (IC₅₀ = 2.9 µM) receptor tyrosine kinases. Does not have any effect on the EGF and IGF receptor tyrosine kinases. Also inhibits the VEGF-driven mitogenesis of human umbilical vein endothelial cells (HUVECs; IC₅₀ ≤ 680 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.

Definition

ChEBI: SU5614 is a member of the class of oxindoles that is 5-chlorooxindole in which the two hydrogens at position 3 are replaced by a (3,5-dimethylpyrrol-2-yl)methylidene group. It has a role as a vascular endothelial growth factor receptor antagonist. It is a member of pyrroles, a member of oxindoles and an organochlorine compound.

Biological Activity

Primary Target
VEGF Flk-1', 'Target IC50: 1.2 μM, 2.9 μM against VEGF (Flk-1) and PDGF receptor tyrosine kinases, respectively; ≤680 nM against the VEGF-driven mitogenesis of human umbilical vein endothelial cells (HUVECs)