Table 1. Bafetinib reverses the ABCB1-mediated drug resistance to doxorubicin and paclitaxel in ABCB1-overexpressing cell lines.
| Treatment | IC50 value ± SDa |
|||
|---|---|---|---|---|
| SW620 (μM, Resistance Foldb) | SW620/Ad300 (μM, Resistance Foldb) | HEK293/pcDNA3.1 (nM, Resistance Foldb) | HEK/ABCB1 (nM, Resistance Foldb) | |
| Doxorubicin | 0.11 ± 0.02 (1.0) | 46.2 ± 2.7 (421.3) | 67.9 ± 4.1 (1.0) | 814.6 ± 122.1 (12.0) |
| + Bafetinib 1 μM | 0.11 ± 0.03 (1.0) | 11.3 ± 1.9 (103.6)* | 53.1 ± 9.3 (0.8) | 537.6 ± 119.3 (7.9)* |
| + Bafetinib 3 μM | 0.08 ± 0.02 (0.7) | 1.7 ± 0.3 (15.4)* | 78.7 ± 6.3 (1.2) | 81.4 ± 35.2 (1.2)* |
| + Verapamil 3 μM | 0.09 ± 0.02 (0.8) | 2.3 ± 0.2 (21.0)* | 72.1 ± 7.0 (1.1) | 137.4 ± 27.1 (2.0)* |
| Paclitaxel | 0.07 ± 0.01 (1.0) | 14.6 ± 2.3 (208.6) | 33.8 ± 2.7 (1.0) | 1352.2 ± 42.2 (40.0) |
| + Bafetinib 1 μM | 0.08 ± 0.01 (1.1) | 5.5 ± 0.8 (78.6)* | 37.9 ± 3.5 (1.1) | 412.2 ± 27.9 (12.2)* |
| + Bafetinib 3 μM | 0.08 ± 0.02 (1.1) | 0.3 ± 0.06 (4.3)* | 44.7 ± 3.3 (1.3) | 58.0 ± 2.6 (1.7)* |
| + Verapamil 3 μM | 0.09 ± 0.02 (1.3) | 0.8 ± 0.1 (11.4)* | 35.2 ± 2.3 (1.0) | 78.6 ± 11.8 (2.3)* |
| Cisplatin | 1.8 ± 0.3 (1.0) | 1.7 ± 0.2 (0.9) | 817.9 ± 96.2 (1.0) | 1153.5 ± 170.6 (1.4) |
| + Bafetinib 1 μM | 1.3 ± 0.1 (0.7) | 1.8 ± 0.1 (1.0) | 865.3 ± 73.7 (1.1) | 971.3 ± 72.5 (1.2) |
| + Bafetinib 3 μM | 1.5 ± 0.1 (0.8) | 1.7 ± 0.2 (0.9) | 840.1 ± 68.2 (1.0) | 933.3 ± 66.4 (1.1) |
| + Verapamil 3 μM | 1.7 ± 0.2 (0.9) | 2.0 ± 0.5 (1.1) | 822.5 ± 69.6 (1.0) | 936.7 ± 51.3 (1.1) |
aIC50 values are represented as mean ± SD of three independent experiments performed in triplicate. bResistance fold was calculated by dividing the IC50 values of substrates in the presence or absence of inhibitor by the IC50 of parental cells without inhibitor.
*p < 0.05 versus no inhibitor group.