compound introduction
Information Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor ofVEGFRwith IC50 of Targets VEGFR2/KDR (HUVECs); c-Kit (HUVECs); c-Kit (HUVECs); VEGFR3/FLT4 (HUVECs); VEGFR1/FLT1 (HUVECs) 29716,0.5 nM; 2 nM; 2 nM; In vitro In recombinant kinase assays, cediranib inhibits VEGFR-1 kinase activity (IC50 = 5 nmol/L) within a similar concentration range to VEGFR-2 and VEGFR-3 (IC50 values of 1 μmol/L) and had marginal activity versus FGFR-1 and -4 (IC50 values of 0.35 and 2.17 μmol/L, respectively). In vivo Phosphorylation of wild-type c-Kit in NCI-H526 tumor xenografts was reduced markedly following oral administration of cediranib (≥1.5 mg/kg/d) to tumor-bearing nude mice.
