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Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC50 values of 77, 37, and 190 nM, respectively.1,2 It less potently inhibits PDGF and c-
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1. New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-
2. A small molecule-
3. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg. Med. Chem. Lett. 13(18), 2967-2971 (2003).
4. Blockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularization. Am. J. Pathol. 156(2), 697-707 (2000).
5. Vascular density analysis in colorectal cancer patients treated with vatalanib (PTK787/ZK222584) in the randomised CONFIRM trials. Br. J. Cancer 107(7), 1044-1050 (2012).