M.W 475.35

Formular C₂₂H₂₄BrFN₄O₂

Solubility Soluble in DMSO at 30 mg/mL

Purity >99%

Biological Activity

Vandetanib is a potent, orally-active inhibitor of kinase insert domain-containing receptor [KDR/vascular endothelial growth factor receptor (VEGFR) 2] tyrosine kinase activity (IC₅₀ = 40 nM). This compound also inhibits fms-like tyrosine kinase 4 (VEGFR3, IC₅₀ = 110 nM) and epidermal growth factor receptor (EGFR/HER1, IC₅₀ = 500 nM) but shows selectivity relating to a range of other tyrosine and serine-threonine kinases. The activity of vandetanib against KDR tyrosine kinase may explain its potent inhibition of vascular endothelial growth factor A-stimulated human umbilical vein endothelial cell proliferation in vitro (IC₅₀ = 60 nM).

Synonym

Caprelsa,Zactima,ZD6474

Store at -20^oC, Desiccate