Table 2.
The effect of olmutinib on drug resistance to MX, SN38, and cisplatin in ABCG2-overexpressing cell lines (NCI-H460 and NCI-H460/MX20, and HEK293/pcDNA3.1 and HEK293/ABCG2).
| Treatment | IC50 ± SDa (RFb) |
|||
|---|---|---|---|---|
| NCI-H460 (nM) | NCI-H460/MX20 (μM) | HEK293/pcDNA3.1 (nM) | HEK293/ABCG2 (μM) | |
| MX | 22.987 ± 4.145(1.00) | 2.327 ± 0.642(101.23) | 72.245 ± 10.834(1.00) | 1.974 ± 0.846(27.32) |
| + Olmutinib (1 μM) | 18.642 ± 4.101(0.81) | 0.039 ± 0.009(1.70)∗∗ | 70.563 ± 20.169(0.98) | 0.261 ± 0.052(3.61)∗ |
| + Olmutinib (3 μM) | 17.067 ± 2.241(0.74) | 0.027 ± 0.017(1.17)∗∗ | 68.125 ± 14.824(0.94) | 0.146 0.038(2.02)∗ |
| + Ko 143 (3 μM) | 16.947 ± 2.643(0.74) | 0.022 ± 0.012(0.96)∗∗ | 62.234 ± 11.216(0.86) | 0.183 ± 0.022(2.53)∗ |
| SN-38 | 13.454 ± 1.156(1.00) | 2.197 ± 0.342(163.30) | 56.462 ± 9.243(1.00) | 2.389 ± 0.279(42.31) |
| + Olmutinib (1 μM) | 12.592 ± 2.392(0.94) | 0.033 ± 0.012(2.45)∗∗ | 56.427 ± 10.421(1.00) | 0.288 ± 0.038(5.10)∗∗ |
| + Olmutinib (3 μM) | 12.346 ± 3.243(0.92) | 0.019 ± 0.034(1.41)∗∗ | 54.364 ± 5.826(0.96) | 0.176 ± 0.029(3.12)∗∗ |
| + Ko 143 (3 μM) | 12.456 ± 4.024(0.93) | 0.021 ± 0.032(1.56)∗∗ | 57.522 ± 8.024(1.02) | 0.164 ± 0.027(2.90)∗∗ |
| IC50 ± SDa (μM) (RFb) | ||||
| Cisplatin | 1.426 ± 0.543(1.00) | 1.745 ± 0.224(1.22) | 1.628 ± 0.252(1.00) | 1.463 ± 0.663(0.90) |
| + Olmutinib (3 μM) | 1.313 ± 0.512(0.92) | 1.654 ± 0.443(1.16) | 1.214 ± 0.478(0.75) | 1.126 ± 0.275(0.69) |
| + Ko 143 (3 μM) | 1.226 ± 0.861(0.86) | 1.494 ± 0.268(1.05) | 1.354 ± 0.368(0.83) | 1.425 ± 0.264(0.88) |
aIC50 values represent the mean ± SD of three independent experiments which were performed in triplicate. bResistance Fold (RF) was calculated by dividing the IC50 values of substrates in the presence or absence of an inhibitor by the IC50 values of parental cells without an inhibitor. ∗P < 0.05, ∗∗P < 0.01 versus no inhibitor group.