Product Name:
CP-673451CAS No.:
343787-29-1
Product Data Sheet
Cat. No.:
HY-12050MWt:
417.50Formula:
C24H27N5O2Purity :
>98%
Solubility:Mechanisms:
Biological Activity:
Pathways:Protein Tyrosine Kinase/RTK; Target:VEGFR DMSO
g y CP-673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM. A dose of 33 mg/kg was adequate to provide >50% inhibition of receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at Cmax. In a sponge angiogenesis model, CP-673451 inhibited 70% of PDGF-BB-stimulated
angiogenesis at a dose of 3 mg/kg (q.d. × 5, p.o., corresponding to 5.5 ng/mL at Cmax). CP-673451did not inhibit vascular endothelial growth factor- or basic fibroblast growth factor-induced angiogenesis at concentrations which inhibited tumor growth.
References:
[1]. Roberts, W. Gregory et al.Antiangiogenic and antitumor activity of a selective PDGFR tyrosine
kinase inhibitor, CP-673,451. Cancer Research (2005), 65(3), 957-966.Caution: Not fully tested. For research purposes only
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