KDR/Flk-1 Kinase Inhibitor IV
3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine
Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV

Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, ATP-competitive inhibitor of VEGFR-2 (KDR/Flk-1; IC₅₀ = 19 nM). 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. Does not inhibit FGFR-1 or Src kinase activity (IC₅₀ > 1.9 µM). Shown to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC₅₀ = 387 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells. Purity: ≥95% by HPLC. CAS 216661-57-3.

Ref.: Cools, J., et al. 2004. Cancer Res. 64, 6385. Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.