CP-673,451 is a selective inhibitor of the platelet-derived growth factor receptor β (PDGFRβ) kinase with an IC50 value of 1 nM. It also inhibits the PDGFRα kinase (IC50 = 10 nM), but exhibits greater than 450-fold selectivity over other angiogenic receptors such as VEGFR 2, TIE-2, and FGR2. In several in vivo tumor models, CP-673,451 has antiangiogenic and antitumor activity.
