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Biological Activity:
A potent and selective inhibitor of tyrosine kinases, targeting VEGFR, with IC50 to be 77 nM (VEGFR-1), 37 nM (VEGFR-2), 580 nM (PDGFR-beta), 730 nM (c-KIT), 660 nM (FLT-4) and 1.4 µM (c-FMS) respectively; not active against EGFR, SRC-ABL and PKC etc.
References: online
JM Wood et al. 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. 2000, 60, 2178-2189.
EN Scott et al. Vatalanib: the clinical development of a tyrosine kinase inhibitor of angiogenesis in solid tumours. Expert Opin Investig Drugs 2007, 16(3), 367–379.
Chemical Name: N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
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