Table 1

Summary of the in vitro activity of SU11248

ReceptorBiochemical Kim)aCellular IC50
Receptor phosphorylation (μm)bLigand-dependent proliferation (μm)c
Flk-1/KDR0.009 ± 0.0020.010.004 ± 0.002
PDGFRβ0.008 ± 0.0030.010.039 ± 0.013
PDGFRαNDdND0.069 ± 0.015
FGFR10.83 ± 0.12ND0.88 ± 0.15
  • a Determined using recombinant enzyme.

  • b Determined after ligand stimulation of serum-starved NIH-3T3 cells engineered to express Flk-1 or PDGFRβ.

  • c Determined using serum-starved HUVECs (KDR and FGFR) or NIH-3T3 cells engineered to express PDGFRα or PDGFRβ

  • d ND, not determined.