Table 1.

In vitro enzymatic inhibitory activity and cellular target activity of SU14813

Target RTKs (biochemical IC50, μmol/L)
Nontarget tyrosine kinases (biochemical IC50, μmol/L)
VEGFR-2VEGFR-1PDGFR-βKITFGFR-1EGFRSrccMet
SU14813
0.05
0.002
0.004
0.015
3.5
>20
2.5
9
Cell target phosphorylation assay (cellular IC50, μmol/L)
Ligand-dependent proliferation (cellular IC50, μmol/L)
Ligand-independent proliferation (cellular IC50, μmol/L)

VEGFR-2
PDGFR-β
KIT
FLT3-ITD
c-fms
PDGF-BB
FL
EGF
FLT3-ITD
SU148130.040.020.0060.050.050.030.07460.02
  • Abbreviations: FGFR-1, FGF receptor 1; FL, FLT3 ligand; EGF, epidermal growth factor.