Table 1

In vitro profile of AEE788 against a panel of kinases

KinaseIC50m] ± SEa
EGFR ICDb0.002 ± 0.0006
ErbB2 (HER-2)0.006 ± 0.0006
ErbB4 (HER-4)0.16 ± 0.026
KDR0.077 ± 0.009
Tek2.1 ± 0.32
IGF1-R>10
Ins-R>10
PDGFR-β0.32 ± 0.038
c-Met2.9 ± 0.38
c-Abl0.052 ± 0.010
c-Src0.061 ± 0.013
c-Kit0.79 ± 0.094
RET0.74 ± 0.03
c-Fms0.060 ± 0.005
Flt-10.059 ± 0.009
Flt-30.73 ± 0.12
Flt-40.33 ± 0.099
Cdk1/Cyc.B8.0 ± 0.79
PKC-α>10
c-Raf-12.8 ± 0.49
PKA>10
  • a Results are expressed as means ± SE; all values are averages of at least three determinations.

  • b EGFR ICD, cloned and purified epidermal growth factor receptor intracellular domain; IGF, insulin-like growth factor; PDGFR, platelet-derived growth factor receptor; Cdk, cyclin-dependent kinase; PKC, protein kinase C; PKA, protein kinase A.