Table 1.

AZD2171 inhibition of VEGF receptor tyrosine kinase activity and selectivity profile

KinaseIC50 (μmol/L) *, mean ± SE
VEGFR family
    KDR (VEGFR-2)<0.001
    Flt-1 (VEGFR-1)0.005 ± 0.002
    Flt-4 (VEGFR-3)≤0.003
PDGFR family
    c-Kit0.002 ± 0.0001
    PDGFR-β0.005 ± 0.001
    PDGFR-α0.036 ± 0.008
    CSF-1R0.11 ± 0.03
    Flt-3>1
Representatives from other kinase families
    FGFR10.026 ± 0.009
    Src0.13 ± 0.02
    Abl0.26 ± 0.05
    EGFR1.6 ± 0.3
    ErbB2 (HER-2/neu)>1
    CDK2>1
    CDK4>1
    Aur-A>10
    Aur-B>10
    MEK>10
  • * The ability of AZD2171 to inhibit human recombinant tyrosine kinase activity was examined with ATP concentrations at, or just below, the respective Km. Data represent the mean ± SE of at least three separate determinations. IC50 values quoted as “greater than” denote the inability to reach an IC50 value with the highest concentration tested.