AdipoGen Vandetanib
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Chemical. CAS 443913-73-3. Formula C22H24BrFN4O2. MW 475.4. Vandetanib is an orally available, ATP mimetic small molecule tyrosine kinases inhibitor that targets vascular endothelial growth factor receptor-2 VEGFR-2, VEGFR-3 and epidermal growth factor receptor EGFR, REarranged during Transfection RET and slightly VEGFR-1. Inhibition of these tyrosine kinases blocks multiple intracellular signaling pathways involved in tumor growth, proliferation, progression and angiogenesis. It inhibits RET, VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRbeta, Tie-2, and FGFR1 in cell-free assays IC50s = 34, 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively. It also binds to 142 additional kinases in a panel of 442 kinases Kds = 4.6-7,900 nM. Vandetanib 1 and 2.5 µM induces apoptosis, autophagy, ROS and cell cycle arrest at the G0/G1 phase and has anti-proliferative properties in several cancer cell lines and in in vivo cancer models.