Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
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Product Description
Information
Cediranib 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.
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 <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 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.
This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
