AZD4547 kinase activity
Kinase | Enzyme IC50,a nmol/L | Cellular IC50, nmol/L |
---|---|---|
FGFR1 | 0.2 ± 0.06 | 12 ± 3 |
FGFR3 | 1.8 ± 0.33 | 40 ± 1 |
FGFR2 | 2.5 ± 0.23 | 2 ± 0.2 |
KDR | 24 ± 0.001 | 258 ± 17 |
FGFR4 | 165 ± 30.3 | 142 ± 29 |
IGFR | 581 ± 0.02 | 828 ± 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.