Table 3.
Effect of ABC transporter modulators on the chemosensitivity of BI 2536 in ABCB1- or ABCG2-overexpressing cell lines
| Cell lines | IC50 (nM)a | ||||
|---|---|---|---|---|---|
|
| |||||
| BI 2536 | BI 2536 + tariquidar (1 μM) | BI 2536 + FTC (3 μM) | BI 2536 + nilotinib (0.5 μM) | BI 2536 + lapatinib (0.3 μM) | |
| KB-3-1 | 1.48 ± 0.53 | 1.35 ± 0.49 | N.D | 0.83 ± 0.40 | 0.89 ± 0.41 |
| KB-V-1 | 281.24 ± 31.57 | 2.09 ± 0.77*** | N.D | 11.44 ± 1.87*** | 11.83 ± 2.41*** |
| S1 | 24.30 ± 4.75 | N.D | 27.18 ± 2.54 | 13.94 ± 2.69* | 25.14 ± 8.11 |
| S1-M1-80 | 261.06 ± 48.25 | N.D | 32.34 ± 12.73** | 18.53 ± 3.03*** | 13.21 ±4.20*** |
| MCF7 | 5.11 ± 1.47 | N.D | 8.37 ± 2.59 | 4.24 ± 1.36 | 9.68 ± 3.19 |
| MCF7-FLV1000 | 393.18 ± 74.83 | N.D | 41.99 ± 28.36** | 124.21 ± 9.57** | 128.31 ± 8.49** |
| pcDNA-HEK293 | 2.75 ± 0.67 | 1.47 ± 0.50 | 2.62 ± 0.72 | 2.13 ± 0.81 | 1.95 ± 0.59 |
| MDR19-HEK293 | 85.50 ± 13.67 | 1.30 ± 0.46*** | N.D | 7.78 ± 1.77*** | 29.61 ± 8.25** |
| R482-HEK293 | 25.97 ± 4.95 | N.D | 3.95 ± 1.43** | 6.26 ± 1.83** | 7.02 ± 2.31** |
Abbreviation: N.D, not determined.
IC50 values are mean ± SD in the presence and absence of BI 2536 or other tested compounds. The IC50 values were calculated from dose-response curves obtained from three independent experiments.
P < 0.05;
P < 0.01;
P < 0.001