VEGFR2 kinase inhibitor IV

VEGFR2 Kinase Inhibitor IV is a 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, ATP-competitive inhibitor of Flk-1 (VEGFR-2/KDR ; IC₅₀ = 19 nM). The compound displays ~2-fold greater selectivity for VEGFR-2 over PDGFRb (IC₅₀ = 34 nM) and 10-fold greater selectivity over VEGFR-1 (Flt-1) and VEGFR-3 (Flt-4; IC₅₀ = 190 nM) tyrosine kinase activity. VEGFR2 Kinase Inhibitor IV does not inhibit FGFR-1 or Src kinase activity (IC₅₀ > 1.9 μM). The chemical has been shown to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC₅₀ = 387 nM). VEGFR2 Kinase Inhibitor IV also inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.