Chemical Name:4-[(4'-Chloro-2'-fluoro)phenylamino]-6,7-dimethoxyquina
zoline hydrochloride
Biological Activity:
Inhibitor of vascular endothelial
growth factor (VEGF) receptor tyrosine kinase. Inhibits activity of KDR and Flt
VEGF receptors (IC50 values are 100 nM and 2 μM
respectively) and displays > 3-fold selectivity over FGFR-1. Orally active
in vivo.
Hennequinet al (1999)
Design and structure-activity relationship of a new class of potent VEGF
receptor tyrosine kinase inhibitors. J.Med.Chem. 42 5369.