In vitro
AZD2171 is a novel indole-ether quinazoline inhibitor. AZD2171, as an ATP-competitive inhibitor, can potently inhibit KDR tyrosine kinase with IC50 less than 1 nM in vitro. AZD2171 are consistent with potent inhibition of VEGF signaling, angiogenesis, neovascular survival, and tumor growth.In human umbilical vein endothelial cells, AZD2171 inhibited VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4 nM and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, AZD2171 also reduced vessel area, length, and branching at subnanomolar concentrations.
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