Table 2 Inhibition of various protein kinases by GW654652

From: Antitumour efficacy of VEGFR2 tyrosine kinase inhibitor correlates with expression of VEGF and its receptor VEGFR2 in tumour models

 

IC50 (μ M)a

Fold selectivity vs VEGFR-2b

VEGFR-2

0.0023±0.0008

—

VEGFR-3

0.0025±0.0005

1.1

VEGFR-1

0.0120±0.0026

5.3

SRC

0.35±0.24

156

Eph-B4

0.46±0.03

204

c-Fms

0.53±0.33

237

Tie2

0.32±0.04

144

EGFR

1.36±0.42

605

ErbB2

11.53±2.74

5125

CDK2

>20

>8800

CDK4

>20

>8800

  1. aValues are mean±s.e.
  2. bRatio for the IC50 obtained with a given kinase compared to that achieved vs VEGFR-2.
  3. VEGFR=vascular endothelial growth factor receptor; IC=inhibitory concentration.
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