CP-547632

CP‑547632 is a small molecule inhibitor developed as an orally bioavailable and selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR‑2) tyrosine kinase. It also potently inhibits basic fibroblast growth factor (FGF) kinases. The drug was discovered by Pfizer in collaboration with OSI Pharmaceuticals. Mechanistically, it blocks VEGF-stimulated autophosphorylation of VEGFR‑2 at nanomolar concentrations and shows selectivity over other related tyrosine kinases such as epidermal growth factor receptor and platelet-derived growth factor beta. Preclinical studies demonstrated inhibition of angiogenesis and tumor growth in vivo. Clinically, it has been investigated for the treatment of various human malignancies including ovarian cancer, lung neoplasms (notably non-small cell lung cancer), peritoneal neoplasms, fallopian tube cancer, and diabetic retinopathy[1][2][3][5].

Other names

3-(4-bromo-2,6-difluorophenyl)methoxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxamide252003–65–9 (CAS number)