Table 1.
The effect of Ko143, a reference inhibitor of ABCG2, on the cytotoxicity of MTX-211 in ABCG2-overexpressing cells.
| Cell Line | Transporter Overexpressed | IC50 ± SD [μM] 1 (R.F. 2) | |
|---|---|---|---|
| MTX-211 | MTX-211 + Ko143 | ||
| S1 | - | 1.24 ± 0.09 (1) | 1.38 ± 0.14 (1) |
| S1-MI-80 | ABCG2 | 21.88 ± 2.32 *** (18) | 2.11 ± 0.26 * (2) |
| H460 | - | 2.97 ± 0.32 (1) | 1.82 ± 0.25 (1) |
| H460-MX20 | ABCG2 | 14.94 ± 2.75 ** (5) | 2.12 ± 0.19 (1) |
| pcDNA3.1-HEK293 | - | 1.36 ± 0.16 (1) | 1.39 ± 0.22 (1) |
| R482-HEK293 | ABCG2 | 27.94 ± 4.45 *** (21) | 7.51 ± 0.90 *** (5) |
Abbreviation: R.F.: resistance factor. 1 IC50 values are mean ± SD calculated from at least three independent experiments, in the presence or absence of 1 μM Ko143. 2 R.F. values were calculated by dividing the IC50 values of MTX-211 in multidrug-resistant cells by the IC50 values of MTX-211 in respective parental cells. * p < 0.05; ** p < 0.01; *** p < 0.001.