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Biological Activity:
A potent and oral tyrosine kinase inhibitor (TKI), targeting VEGFR-2 and basic FGF kinases (IC50 to be 11 and 9 nM respectively); selective relative to EGFR, PDGF-ß, and other related TKs; inhibits VEGF-stimulated autophosphorylation
of VEGFR-2 in a whole cell assay with an IC50 value of 6 nM.
References:
JS Beebe et al. Pharmacological Characterization of CP-547,632, a Novel Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitor for Cancer Therapy. Cancer Res. 2003, 63, 7301-7309. [online]
Chemical Name: 3-[(4-Bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide
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