CP-673451 is a potent, selective, orally acitve PDGFR inhibitor with IC50 of 1 and 10 nM for PDGFR-α and PDGFR-β, respectively.
CP-673451 inhibits PDGFR-β autophosphorylation with IC50 of 1 nM in cell-based assyas, displays >450-fold selectivity over other angiogenic receptors, including VEGFR-1, VEGFR-2, TIE-2, and FGFR-2.
CP-673451 inhibits PDGFR phosphorylation in tumor xenografts and inhibits multiple types tumor growth in vivo.
CP-673451 also robustly inhibits centrosome clusterin, induces mitotic spindle multipolarity by activation of the actin-severing protein cofilin in cancer cells.
