Inhibitory activities of lenvatinib and metabolites on the phthalazine oxidation activity of AO
Data represent the mean of triplicate determinations.
| Inhibitora | Concentration | Remaining Activity (% of control) | IC50 |
|---|---|---|---|
| μM | μM | ||
| Control | 0 | 100.0 | NA |
| Lenvatinib | 100 | 63.8 | >100 |
| 10 | 84.9 | ||
| M2 | 100 | 38.8 | 11.6 |
| 10 | 55.4 | ||
| M3 | 100 | 30.4 | 30.8 |
| 10 | 46.2 | ||
| M2′ | 100 | 109.5 | >100 |
| 10 | 100.5 | ||
| M3′ | 50 | 95.0 | >50 |
| 10 | 98.1 | ||
| Raloxifene | 0.01 | 14.5 | 0.0035 |
| 0.001 | 82.5 |
NA, not analyzed.
↵a Concentration of phthalazine as substrate is 10 μM.