Table 1.

PF-03814735 and its kinase inhibitory properties

graphic
KinaseIC50, nmol/L% Inhibition
Aurora10.8 ± 0.6nd
Aurora25 ± 3≥90
Flt110≥90
FAK22nd
TrkA30≥90
Met100≥90
FGFR1100≥90
CDK5/p35nd≥90
Flt3(D835Y)nd≥90
ARK5nd≥90
NEK2nd≥90
Flt4nd≥90
Retnd≥90
MLK1nd≥90
TrkBnd≥90
Fernd≥90
JAK2nd≥90
Flt3nd≥90
MST3nd≥90
CDK5/p25nd≥90
MST2nd≥90
Rsk3nd≥90
Abl(T315I)nd69
Ablnd50

NOTE: The chemical structure of the trifluoromethylpyrimidine PF-03814735. The kinase inhibition profile was assessed against a panel of 220 recombinant protein kinases at 100 nmol/L concentration of PF-03814735 and ATP substrate at 10 μmol/L. Kinases that showed ≥90% inhibition are indicated, except for the Abl kinase, which showed 50% inhibition. For a subset of kinases, additional concentrations of PF-03814735 were evaluated to calculate the IC50 value (± SD when available).

Abbreviation: nd, not done.