Cediranib maleate is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM. It also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM. It inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM in vitro. It suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. It even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis in vivo. It causes hypertrophy in bone growth plate and prevents luteal development in ovary. It shows broad spectrum activity in human tumor models at doses that are well tolerated. It causes regression of vascular tissues in human lung tumor xenografts.
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