Description
Vandetanib (ZD6474) can inhibit VEGFR2 with IC50 of 40 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C22H24BrFN4O2
Chemical Name
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
Solubility
DMSO 4 mg/mL Water
In vitro
As a novel, orally available, ATP mimetic small molecule inhibitor, Vandetanib (ZD6474) inhibits vascular endothelial growth factor receptor (VEGFR)-2, fms-like tyrosine kinase 4(VEGFR-3), and epidermal growth factor receptor (EGFR) with IC50 of 40 nM, 110 nM and 500 nM. Vandetanib (ZD6474) is also an inhibitor of REarranged during Transfection (RET) tyrosine kinases and Vandetanib (ZD6474) can inhibit RET-derived oncoproteins around 100 nM. Vandetanib (ZD6474) can block cell proliferation of human umbilical vein endothelial cell which is stimulated by vascular endothelial growth factor-A with IC50 of 60 nM.
In vivo
In vivo, mice in the vandetanib group had tumor volumes significantly lower than those in the control group. Vandetanib induce an increase in apoptosis of both tumor cells and endothelial cells within the tumor xenografts. Animals were treated for 28 days with 1 mg/kg/d (DTX1) or 6 mg/kg q4d (DTX6) docetaxel with or without vandetanib (15 mg/kg/d p.o.) in mice bearing UMSCC2 tumor xenografts. Docetaxel with vandetanib is effective in treating UMSCC2 xenografts at concentrations relevant to exposures in humans.
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