Table 2. Inhibition of various protein kinases by GW654652.
| IC50 (μM)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 |
a
Values are mean±s.e.
b
Ratio for the IC50 obtained with a given kinase compared to that achieved vs VEGFR-2.
VEGFR=vascular endothelial growth factor receptor; IC=inhibitory concentration.