Table 1.

AZD4547 kinase activity

KinaseEnzyme IC50,a nmol/LCellular IC50, nmol/L
FGFR10.2 ± 0.0612 ± 3
FGFR31.8 ± 0.3340 ± 1
FGFR22.5 ± 0.232 ± 0.2
KDR24 ± 0.001258 ± 17
FGFR4165 ± 30.3142 ± 29
IGFR581 ± 0.02828 ± 41
AXL>2,000
CDK2>10,000
FAK>10,000
ROCK2>50,000
AKT1>100,000
ALK1>100,000
p38>100,000
PI3Ka>100,000
  • aThe ability of AZD4547 to inhibit a range of human recombinant kinase activities was tested using ATP concentrations at, or just below, the respective Km. Data represent the mean ± SEM of at least 3 separate determinations. IC50 values denoted as “greater than” denote the inability to reach 50% inhibition of maximal activity at the highest tested concentration.