Table 2.
Effect of crizotinib on reversing ABCB1- mediated MDR in transfected cell lines
| IC50± SD (µM) (fold-reversal) | ||||
|---|---|---|---|---|
| Compounds | HEK293 | HEK293/ABCB1 | ||
| Doxorubicin | 0.058 ± 0.001 | (1.00) | 0.643 ± 0.013 | (1.00) |
| +0.375 µM Crizotinib | 0.063 ± 0.009 | (0.91) | 0.367 ± 0.021** | (1.75) |
| +0.75 µM Crizotinib | 0.056 ± 0.007 | (1.03) | 0.244 ± 0.059** | (2.64) |
| +1.5 µM Crizotinib | 0.046 ± 0.008 | (1.25) | 0.133 ± 0.030** | (3.87) |
| +10 µM Verapamil | 0.044 ± 0.006 | (1.32) | 0.049 ± 0.008** | (13.1) |
| Paclitaxel | 0.039 ± 0.002 | (1.00) | 0.8137 ± 0.098 | (1.00) |
| +0.375 µM Crizotinib | 0.035 ± 0.004 | (1.11) | 0.488 ± 0.160** | (1.67) |
| +0.75 µM Crizotinib | 0.034 ± 0.004 | (1.15) | 0.334 ± 0.079** | (2.43) |
| +1.5 µM Crizotinib | 0.033 ± 0.003 | (1.18) | 0.195 ± 0.035** | (4.16) |
| +10 µM Verapamil | 0.031 ± 0.003 | (1.26) | 0.055 ± 0.007** | (18.0) |
| Cisplatin | 2.014 ± 0.341 | (1.00) | 2.281 ± 0.046 | (1.00) |
| +1.5 µM Crizotinib | 1.989 ± 0.360 | (1.18) | 2.360 ± 0.058 | (0.96) |
| +10 µM Verapamil | 2.380 ± 0.081 | (1.26) | 2.032 ± 0.083 | (1.12) |
Cell survival was determined by MTT assays. Data are the means ± SD of at least three independent experiments performed in triplicate. The fold reversal of MDR (values given in parentheses) was calculated by dividing the IC50 for cells with the anticancer drugs in the absence of inhibitor by that obtained in the presence of inhibitor.
**
P < 0.01, significantly different from values obtained in the absence of inhibitor.