TABLE 2

The effect of dialysis on the preincubation-dependent inactivation of CYP2C8 by bosutinib (150 µM) and of CYP3A by lestaurtinib (200 µM) and saracatinib (64 µM)

Each experiment is compared with its own control, that is, either preincubation without inhibitor or preincubation without inhibitor, followed by dialysis (3 ☓ 2 h at 4°C). In the experiments, human liver microsomes (HLM) (0.5 mg/ml) and NADPH were preincubated with or without inhibitor for 30 min. The samples were immediately dialyzed against sodium phosphate buffer three times for 2 h, followed by a 20-fold dilution and measurement of CYP2C8 or CYP3A4 activity. Values are expressed as mean ± S.D. of duplicates or more.