Potent VEGFR inhibitor (IC50 values are 37 and 77 nM for VEGFR-2 and -1, respectively). Inhibits proliferation, migration and survival of HUVECs in vitro and inhibits growth, vascularization and metastasis of tumors expressing VEGFR in mouse models. Also inhibits PDGFR-β, c-Kit and c-Fms. Potent aromatase inhibitor (IC50 = 50 nM). Orally available.
Banerjee et al (2009) The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase. Cancer Res. 69 4716 PMID:19435899 |Wood et al (2000) PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 60 2178 PMID:10786682 |Bold et al (2000) New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J.Med.Chem. 43 2310 PMID:10956229