TABLE 2

IC50 values for in vitro selectivity of JNJ-17029259 and other VEGF-R2 kinase inhibitors

Kinase JNJ-17029259 SU-5416 ZD-6474 PTK787
μM
VEGF-R1 0.090 ± 0.009 0.043a 0.90a 0.077c
VEGF-R3 0.012 ± 0.003 0.050a 0.233a 0.195a
Tie2 1.95 ± 0.07 >10a 0.567a >10c
PDGF-Rβ 0.27 ± 0.09 2.22a 0.477a 0.580c
FGF-R1 0.10 ± 0.02 >10a 2.31a >10c
FGF-R2 0.172 ± 0.004
FLT3 0.23 ± 0.05
c-kit >100 0.660a 0.343a 0.730c
CDK1:cyclin B 4.80 ± 0.41 >10a >10a >10c
EGF-R >100 >10a 0.016a >10c
HER2 2.09 ± 0.57 >20b
Protein kinase-A >100
Protein kinase-Cγ 28.3 ± 2.88
Protein kinase-Cβ2 >100
Casein kinase-1 36.76 ± 0.88
Casein kinase-2 >100
Calmodulin kinase-2 24.52 ± 1.97
GSK3β 1.31 ± 0.1
ERK2 (MAP kinase) >100
Insulin-R kinase β >100

  • ↵ a Data from Manley et al. (2002).

  • ↵ b Data from Wedge et al. (2002).

  • ↵ c Data from Wood et al. (2000).