TABLE 1

In vitro potency of PF-670462 and literature standards

Data represent the mean ± S.E.M. for n = 3 to 5 determinations.




CKI∈ Inhibitiona (IC50)

PER3 Nuclear Translocationb (EC50)
nM
PF-670462 7.7 ± 2.2 290 ± 39
IC261 30,700 ± 2280 N.D.
CKI-7 35,600 ± 3670 N.D.
D4476
270 ± 106
7610 ± 285
  • N.D., not determined; indicates that solubility and/or toxicity issues prevented reliable determination of an EC50 value.

  • a Kinase-Glo assay (see Materials and Methods).

  • b ArrayScan (Cellomics) (see Materials and Methods).