TABLE 2

Kinase selectivity of PF-670462 as determined in a broad panel screen


IC50 > 30 μMa (>3000-Fold Selective)

30 μM > IC50 > 3.0 μM (300- to 3000-Fold Selective)

3.0 μM > IC50 > 0.3 μM (30- to 300-Fold Selective)

IC50 < 0.3 μMb (<30-Fold)
AKT1 ABL LCK CKIδ (14 nM; 1.8-fold)
CAMK1 Aurora A MAP3K9 EGFR (150 nM; 19-fold)
CDK2 BTK MAP4K4 SAPK2A/p38 (190 nM; 25-fold)
CDK6 CK2 PKA
CHK1 CLK1 TRK-A
CHK2 ECK
IKKβ FGFR1
IKKi GSK3β
INSR MST2
JAK3 MYLK2
MAPK1/ERK2 PKCβII
MAPKAP SRC
MARK1 TAOK3
MASK VEGFR2
MET
NEK2
PAK4
PDK1
PIM2
PKCζ
ROCK1
S6K
SGK



  • IKK, Iκ B kinase complex; MAPKAP, mitogen-activated protein kinase-activated protein; MASK, Mst3 and SOK1-related kinase; MET, Met proto-oncogene tyrosine kinase; SGK, serum and glucocorticoid-inducible kinase; ABL, abl proto-oncogene kinase; BTK, Bruton's tyrosine kinase; ECK, eck receptor protein tyrosine kinase; SRC, src tyrosine kinase; LCK, lck tyrosine kinase; TRK-A, trkA tyrosine kinase.

  • a Selectivity determinations are based on a -fold ratio of the IC50 value for CKI∈ relative to that observed for other kinases. For example, with a potency of 7.7 nM for CKI∈, activity for other kinases with potency values of >30 μM would yield >3000-fold selectivity for PF-670462.

  • b IC50 value and CKI∈ selectivity are shown in parentheses.