Chemical Name:5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methyl
phenol hydrochloride
Biological Activity:
Potent and selective inhibitor of human vascular
endothelial growth factor receptor 2 (VEGFR-2/KDR) activity. Selectively
inhibits VEGFR-2 (IC50 = 2 nM) over VEGFR-1 and a range of other
receptor tyrosine kinases such as PDGFRβ, FGFR1, EGFR
and erbB2 (IC50 > 50 μM). Inhibits
VEGF-A-induced endothelial cell proliferation in vitro (IC50 = 8
nM).
Whittleset
al (2002) ZM323881, a novel inhibitor of vascular endothelial growth
factor-receptor-2 tyrosine kinase activity. Microcirculation 9 513. Endo
et al (2003) Selective inhibition of vascular endothelial growth factor
receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 in human aortic
endothelial cell responses to VEGF. J.Recept.Signal Transduct.Res. 23
239.