Cediranib Maleate (C09-0823-013)

InformationCediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor ofVEGFRwith IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.TargetsVEGFR2/KDR (HUVECs); c-Kit (HUVECs); c-Kit (HUVECs); VEGFR3/FLT4 (HUVECs); VEGFR1/FLT1 (HUVECs) 29716,0.5 nM; 2 nM; 2 nM; <=3 nM; 5 nMIn vitroIn 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 <0.1 and ≤3 nmol/L). It shows selectivity against other kinases. Cediranib has similar potency against c-Kit when compared with VEGFR-2 in phosphorylation assays but less potency against PDGFR-α and PDGFR-β, particularly in a PDGF-AA/PDGFR-α–driven tumor cell proliferation assay. Cediranib is inactive against wild-type Flt-3 (IC50 value >1 μmol/L) and had marginal activity versus FGFR-1 and -4 (IC50 values of 0.35 and 2.17 μmol/L, respectively).In vivoPhosphorylation 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. Specification: 0.97 Molecular Formula: C25H27FN4O3.C4H4O4 Molecular Weight: 566.58 PubChem CID: 11226834 Isomeric SMILES: CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5.C(=C/C(=O)O)/C(=O)O