Table 2.
The effect of selected RTKIs on VEGF-stimulated firefly luciferase production in VEGFR2 NFAT cells
| Inhibition of 1 nM VEGF165a pIC50 | n | Inhibition of 3 nM VEGF165b pIC50 | n | Reported binding pKD for purified kinase domain* | |
|---|---|---|---|---|---|
| Cediranib | 9.13 ± 0.01 | 5 | 9.38 ± 0.07 | 5 | 8.96 |
| Pazopanib | 8.25 ± 0.03 | 5 | 8.29 ± 0.10 | 8 | 7.85 |
| Sorafenib | 8.01 ± 0.06 | 5 | 7.96 ± 0.04 | 5 | 7.23 |
| Vandetanib | 6.72 ± 0.03 | 5 | 7.00 ± 0.04 | 6 | 6.08 |
VEGFR2 NFAT cells were treated with each RTKI and either 1 nM VEGF165a or 3 nM VEGF165b. Data are mean ± SEM of n separate experiments. Each individual experiment was performed in quadruplicate. Individual fitted values for pIC50 values were obtained in each individual experiment and then analysed to provide mean ± SEM data provided here.
*
Values taken from Davis et al., 2011.