Inhibitor of the VEGFR-2 and FGFR1 kinases
     
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Inhibitor of the VEGFR-2 and FGFR1 kinases

3-[(4-Bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide (CP-547632)
potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 = 11 and 9 nM, respectively). It is selective relative to epidermal growth factor receptor, platelet-derived growth factor , and other related TKs. It also inhibits VEGF-stimulated autophosphorylation of VEGFR-2 in a whole cell assay with an IC50 value of 6 nM

Inhibitor_of_the_VEGFR-2_and_basic_fibroblast_growth_factor_FGF_kinases
OTAVAchemicals Catalogue Number: 1156353
CAS Registry Number: 252003-65-9
Purity: 95%+ (HPLC)


Ref.: Beebe et al. Pharmacological Characterization of CP-547,632, a Novel Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitor for Cancer Therapy. Cancer Research (2003), 63, 7301-7309


Abstract: CP-547,632 is a well-tolerated, orally-bioavailable inhibitor presently under clinical investigation for the treatment of human malignancies.

http://cancerres.aacrjournals.org/cgi/reprint/63/21/7301.pdf

 
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