Abstract
(+/-)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in rodent models of angiogenesis upon oral administration.
MeSH terms
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Administration, Oral
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Angiogenesis Inhibitors / chemical synthesis
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Angiogenesis Inhibitors / metabolism
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Corneal Neovascularization / drug therapy
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Female
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Humans
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Immunoblotting
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Mice
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Mice, Inbred C57BL
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Mice, Nude
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / pharmacokinetics
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Protein Kinase Inhibitors / pharmacology*
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Protein-Tyrosine Kinases / antagonists & inhibitors*
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Pyrimidinones / chemical synthesis
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Pyrimidinones / pharmacokinetics
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Pyrimidinones / pharmacology*
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Rats
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Rats, Wistar
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Receptors, Fibroblast Growth Factor / antagonists & inhibitors
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Receptors, Platelet-Derived Growth Factor / antagonists & inhibitors
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Tumor Cells, Cultured
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Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors
Substances
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Angiogenesis Inhibitors
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Protein Kinase Inhibitors
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Pyrimidinones
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RO4383596
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Receptors, Fibroblast Growth Factor
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Protein-Tyrosine Kinases
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Receptors, Platelet-Derived Growth Factor
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Vascular Endothelial Growth Factor Receptor-2