Table 1.
Effect of tyrosine kinase inhibitors on different markers of toxicity.
| HepG2 (AK release) |
HepG2 (ATP content) |
HepaRG (AK release) |
HepaRG (ATP content) |
Glycolysis (HepG2 cells) | MMP (HepG2 cells) | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 6 h | 24 h | 48 h | 6 h | 24 h | 48 h | Induced | Non-induced | Induced | Non-induced | |||
| Erlotinib | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Imatinib | >100 | >100 | >100 | >100 | 44.0 | 39.4 | >100 | >100 | 62.8 | 58.7 | 61.4 | 59.8 |
| Lapatinib | >50 | 46.7 | 33.2 | >50 | 34.4 | 24.1 | >50 | >50 | >50 | >50 | >50 | 27.5 |
| Sunitinib | >50 | 43.6 | 14.0 | 39.4 | 23.5 | 20.1 | 45.3 | 48.0 | 37.3 | 37.5 | 34.4 | 16.3 |
EC50 values were calculated using GraphPad Prism 6 as described in Methods based on the data provided in the corresponding figures. Incubation times in HepG2 cells for AK release and ATP content were as indicated and 48 h for HepaRG cells, glycolysis and the MMP. Units are μM. AK, Adenylate kinase; MMP, mitochondrial membrane potential.