Table 1.
The effect of olmutinib on drug resistance to paclitaxel, vincristine, and cisplatin in ABCB1-overexpressing cell lines (KB-3-1 and KB-C2, HEK293/pcDNA3.1, and HEK293/ABCB1).
| Treatment | IC50 ± SDa (RFb) |
|||
|---|---|---|---|---|
| KB-3-1 (μM) | KB-C2 (μM) | HEK293/pcDNA3.1 (μM) | HEK293/ABCB1 (μM) | |
| Paclitaxel | 0.034 ± 0.007(1.00) | 2.389 ± 0.541(70.26) | 0.173 ± 0.072(1.00) | 4.464 ± 0.466(25.80) |
| + Olmutinib (1 μM) | 0.038 ± 0.009(1.12) | 2.237 ± 0.487(65.79) | 0.158 ± 0.025(0.91) | 3.653 ± 1.096(21.12) |
| + Olmutinib (3 μM) | 0.036 ± 0.007(1.06) | 2.174 ± 0.641(63.94) | 0.134 ± 0.074(0.77) | 3.462 ± 0.981(20.01) |
| + Verapamil (3 μM) | 0.054 ± 0.016(1.59) | 0.495 ± 0.144(14.56)∗∗ | 0.153 ± 0.146(0.88) | 0.263 ± 0.034(1.52)∗∗ |
| Vincristine | 0.028 ± 0.006(1.00) | 1.299 ± 0.361(46.39) | 0.086 ± 0.221(1.00) | 0.763 ± 0.647(8.87) |
| + Olmutinib (1 μM) | 0.024 ± 0.006(0.86) | 1.217 ± 0.389(43.46) | 0.071 ± 0.016(0.83) | 0.733 ± 0.068(8.52) |
| + Olmutinib (3 μM) | 0.021 ± 0.007(0.75) | 1.132 ± 0.238(40.43) | 0.063 ± 0.017(0.73) | 0.651 ± 0.692 (7.57) |
| + Verapamil (3 μM) | 0.032 ± 0.015(1.14) | 0.056 ± 0.011(2.00)∗∗ | 0.077 ± 0.013(0.90) | 0.126 ± 0.051(1.47) |
| Cisplatin | 1.194 ± 0.876(1.00) | 1.863 ± 0.428(1.56) | 1.523 ± 0.285(1.00) | 1.945 ± 0.876(1.28) |
| + Olmutinib (3 μM) | 1.123 ± 0.473(0.94) | 1.346 ± 0.283(1.13) | 1.433 ± 0.465(0.94) | 1.683 ± 0.464(1.11) |
| + Verapamil (3 μM) | 1.744 ± 0.452(1.46) | 1.643 ± 0.233(1.38) | 1.245 ± 0.337(0.82) | 1.534 ± 0.344(1.01) |
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 < 0.01 versus no inhibitor group.