Table 1.

Kinase inhibition profile of ABT-869

Related RTK*
Nonrelated TK*
Serine/threonine kinases
KinaseIC50 (nmol/L)KinaseIC50 (nmol/L)KinaseIC50 (nmol/L)
KDR4SRC>50,000AKT>50,000
FLT13IGFR>50,000SGK940
FLT4190INSR>50,000CDC29,800
PDGFRβ66LCK38,000PKA5,900
CSF-1R3EGFR>50,000
KIT14HCK>50,000
FLT34CMET>50,000
TIE2170LYN>20,000
RET1,900FYN>50,000
FGFR>12,500FGR>50,000
  • * IC50s determined at an ATP concentration of 1 mmol/L.

  • IC50s determined at an ATP concentration of 5 to 10 μmol/L.