Inhibition potency of selected kinase inhibitors against the formation of 6α-hydroxypaclitaxel and p-3′-hydroxypaclitaxel
| Inhibitors | Reversible Kia (µM) | |
|---|---|---|
| 6α-Paclitaxel Hydroxylation (CYP2C8) | p-3′-Paclitaxel Hydroxylation (CYP3A4) | |
| Afatinib | 94.83 ± 27.05 | 53.38 ± 19.76 |
| Axitinib | 0.17 ± 0.07 | 1.94 ± 1.10 |
| Bosutinib | 1.94 ± 0.24 | 0.14 ± 0.06 |
| Dasatinib | 6.31 ± 1.44 | 2.29 ± 1.63 |
| Erlotinib | 4.02 ± 0.56 | 1.28 ± 0.07 |
| Gefitinib | 8.69 ± 0.47 | 4.80 ± 5.04 |
| Imatinib | 11.28 ± 0.97 | 7.68 ± 2.29 |
| Lapatinib | 1.43 ± 0.73 | 3.83 ± 0.81 |
| Nilotinib | 0.10 ± 0.01 | 0.28 ± 0.34 |
| Pazopanib | 3.72 ± 0.49 | 0.97 ± 0.26 |
| Sorafenib | 1.59 ± 0.38 | 4.11 ± 2.13 |
| Sunitinib | 91.51 ± 27.38 | 20.35 ± 8.74 |
↵a Reversible inhibitory Ki values were determined as described in Materials and Methods. The inhibitor concentrations used were 0.04, 0.2, 0.5, 1, 2, 5, 10, 50, and 100 μM, along with paclitaxel concentrations of 2.5, 5, and 10 μM. The average of three separate incubations was reported.