| Description |
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC 50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC 50 = 1.24 nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive "DFG-out" conformation, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC 50 = 236, 380, 640, and 2820 nM, respectively) and displaying little or no activity against EGFR/HER-1/ErbB (IC 50 = 10.4 µM) and six other kinases (IC 50 ≥10 µM)
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