TABLE 2.
Effects of neratinib in reversing ABCB1-mediated MDR in transfected cell lines
Cell survival rates were determined with MTT assays, as described under Materials and Methods. Data are the mean ± S.D. of at least three independent experiments performed in triplicate. The fold reversal of MDR was calculated by dividing the IC50 for cells with the anticancer drug in the absence of inhibitor by that in the presence of inhibitor.
| Compounds | IC50 (Reversal) |
|
|---|---|---|
| HEK293/pcDNA3.1 | HEK293/ABCB1 | |
| μM (fold) | ||
| Doxorubicin | 0.074 ± 0.006 (1.00) | 1.339 ± 0.130 (1.00) |
| + 0.25 μM Neratinib | 0.065 ± 0.006 (1.13) | 0.756 ± 0.070 (1.77)** |
| + 0.5 μM Neratinib | 0.079 ± 0.008 (0.94) | 0.332 ± 0.027 (4.03)** |
| + 1.0 μM Neratinib | 0.082 ± 0.007 (0.90) | 0.167 ± 0.010 (7.98)** |
| + 10 μM Verapamil | 0.083 ± 0.008 (0.89) | 0.094 ± 0.008 (14.19)** |
| Cisplatin | 2.431 ± 0.27 (1.00) | 2.681 ± 0.27 (1.00) |
| + 1.0 μM Neratinib | 2.263 ± 0.22 (1.07) | 2.176 ± 0.22 (1.23) |
| + 10 μM Verapamil | 2.356 ± 0.23 (1.03) | 2.344 ± 0.23 (1.14) |
P < 0.01 versus the values obtained in the absence of inhibitor.