Biochem/physiol Actions

Cediranib (AZD2171) is an orally active anticancer agent and a highly potent ATP-competitive receptor tyrosine kinase (RTK) inhibitor against VEGFR (IC₅₀ = 5 nM/Flt-1 (VEGFR1), ﹤1 nM/KDR (VEGFR2), ≤3 nM/Flt-4 (VEGFR3), c-Kit (IC₅₀ = 2 nM), PDGFR1/2 (IC₅₀ = 5/36 nM), and FGFR1 (IC₅₀ = 26 nM). Cediranib exhibits reduced activity against CSF-1R, Src, Abl (IC₅₀ = 110, 130, 260 nM, respectively) and little or no potency toward Flt-3, EGFR, ErbB2 (Her-2/neu), CDK2/4, Aurora A/B, and MEK.