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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.
Ordering Information
Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
VEGFR2 kinase inhibitor IV, 1 mg | sc-204381 | 1 mg | $200.00 |