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Description: Vandetanib hydrochloride (formerly also known as ZD6474) is a novel, highly potent, orallybioavailable, selective inhibitor of VEGFR2 with IC50 of 40 nM in acell-free assay. Vandetanib selectively inhibits the tyrosine kinaseactivity of vascular endothelial growth factor receptor 2 (VEGF2), thereby blocking VEGF-stimulated endothelial cell proliferation andmigration and reducing tumor vessel permeability. The inhibition ofVEGFR-2 was 2.7-fold more potent than that of VEGFR-3 (Flt-4) kinase and40-fold more potent than that of VEGFR-1. In human umbilical veinendothelial cells, treatment of ZD6474 resulted in significantinhibition of cell proliferation stimulated by VEGF and EGF with IC50values of 60 and 170 nM, respectively.
References: Cancer Res. 2002 Aug 15; 62(16):4645-55; Clin Cancer Res. 2012 Jul 15; 18(14):3924-33; Clin Cancer Res. 2003 Apr; 9(4):1546-56.
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