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Description

A cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC50 = 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC50 = 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC50 >3 µ,M) and 47 other protein kinases. Inhibits VEGF-induced (IC50 = 10 nM), but not bFGF-induced (IC50 >3 µ,M) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED50 = 2.1 mg/kg, b.i.d, p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h, Cmax = 787 ng/ml).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC50 = 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC50 = 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC50 >3 µ,M) and 47 other protein kinases. Inhibits VEGF-induced (IC50 = 10 nM), but not bFGF-induced (IC50 >3 µ,M) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED50 = 2.1 mg/kg, b.i.d, p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h, Cmax = 787 ng/ml).