Vandetanib
Fumarate (formerly also known as ZD6474) is a novel, highly potent, orally
bioavailable, selective inhibitor of VEGFR2 with IC50 of 40 nM in a
cell-free assay. Vandetanib selectively inhibits the tyrosine kinase
activity of vascular endothelial growth factor receptor 2 (VEGF2),
thereby blocking VEGF-stimulated endothelial cell proliferation and
migration and reducing tumor vessel permeability. The inhibition of
VEGFR-2 was 2.7-fold more potent than that of VEGFR-3 (Flt-4) kinase and
40-fold more potent than that of VEGFR-1. In human umbilical vein
endothelial cells, treatment of ZD6474 resulted in significant
inhibition of cell proliferation stimulated by VEGF and EGF with IC50
values of 60 and 170 nM, respectively.
纯度:≥98%
CAS:338992-00-0