VEGFR Tyrosine Kinase Inhibitor III, KRN633

VEGFR Tyrosine Kinase Inhibitor III, KRN633 is a cell-permeable, reversible, ATP-competitive inhibitor of VEGFR kinase activity (IC₅₀ = 170 nM, 160 nM, and 125 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively). Inhibits PDGFR-α and c-Kit at higher concentrations only (IC₅₀ = 0.97 µM and 4.33 µM, respectivly) and inactive towards 17 other kinases (IC₅₀ ≥ 10 µM). Shown to suppress VEGF-dependent, but not FGF-dependent, cellular signaling and cell proliferation. Although not cytotoxic to cancer cells, KRN633 exhibits excellent antitumor activity due to its inhibitory effects on vessel formation and vascular permeability.