Chemical Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate
Biological ActivityPotent 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase.
Banerjee et al.
Cancer Res., 2009;69:4716
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.
Wood et al.
Cancer Res., 2000;60:2178
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Bold et al.
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