Catalog Number: 5680
Alternate Names: CGP 79787D, PTK787/ZK222584
Chemical Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate
Biological Activity
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.
Technical Data
  • M.Wt:
    464.9
  • Formula:
    C20H15ClN4.C4H6O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    212142-18-2
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.
Background References
  1. The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase.
    Banerjee et al.
    Cancer Res., 2009;69:4716
  2. 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
  3. 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.
    J.Med.Chem., 2000;43:2310

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