Table 2.
Effect of rociletinib on reversing ABCG2-mediated MDR in stable-transfected cells.
| Compound | IC50 ± SD (μmol/L) (fold-reversal) |
||
|---|---|---|---|
| HEK293/pcDNA3.1 | ABCG2-482-R2 | ABCG2-482-T7 | |
| MX | 0.0074 ± 0.0029 (1.00) | 0.0591 ± 0.0133 (1.00) | 0.0279 ± 0.0085 (1.00) |
| +0.25 μmol/L Rociletinib | 0.0052 ± 0.0014 (1.42) | 0.0269 ± 0.0089 (2.20)** | 0.0133 ± 0.0033 (2.10)** |
| +0.5 μmol/L Rociletinib | 0.0062 ± 0.0064 (1.19) | 0.0179 ± 0.0034 (3.30)** | 0.0074 ± 0.0010 (3.77)** |
| +1 μmol/L Rociletinib | 0.0055 ± 0.0014 (1.35) | 0.0119 ± 0.0048 (4.97)** | 0.0072 ± 0.0025 (3.88)** |
| +2.5 μmol/L FTC | 0.0093 ± 0.0030 (0.80) | 0.0047 ± 0.3193 (12.57)** | 0.0118 ± 0.0053 (2.36)** |
| DDP | 2.2131 ± 0.4176 (1.00) | 0.9374 ± 0.2273 (1.00) | 0.7426 ± 0.1449 (1.00) |
| +1 μmol/L Rociletinib | 1.9302 ± 0.2961 (1.15) | 0.7982 ± 0.1226 (1.17) | 0.8032 ± 0.2545 (0.92) |
Cell survival was performed by MTT assay as described in “Materials and methods”. FTC (specific inhibitor of ABCG2) was used as the positive control. The fold reversal of MDR (values given in parentheses) was calculated by dividing the IC50 value for cells with the anticancer agent in the absence of rociletinib by that obtained in the presence of rociletinib. Data were shown as the mean ± SD of at least three independent experiments performed in triplicate. *P < 0.05, **P < 0.01.