Table 2.
Cytotoxicity of SIS3 in human cancer cell lines overexpressing ABCB1 or ABCG2.
| Cell line | Type | Transporter expressed |
IC50 (nM)† | R.F‡ |
|---|---|---|---|---|
| KB-3–1 | epidermal | - | 10.73 ± 4.14 | 1.0 |
| KB-V-1 | epidermal | ABCB1 | 9.56 ± 3.70 | 0.9 |
| OVCAR-8 | ovarian | - | 7.58 ± 1.07 | 1.0 |
| NCI-ADR-RES | ovarian | ABCB1 | 8.79 ± 1.77 | 1.2 |
| H460 | lung | - | 9.97 ± 3.53 | 1.0 |
| H460-MX20 | lung | ABCG2 | 8.30 ± 2.12 | 0.8 |
| S1 | colon | - | 4.06 ± 0.93 | 1.0 |
| S1-M1–80 | colon | ABCG2 | 3.54 ± 0.48 | 0.9 |
| MCF7 | breast | - | 8.90 ± 2.22 | 1.0 |
| MCF7-FLV1000 | breast | ABCG2 | 11.21 ± 1.72 | 1.3 |
| MCF7-AdVp3000 | breast | ABCG2 | 10.11 ± 2.79 | 1.1 |
Abbreviation: RF, resistance factor.
† IC50 values are mean ± SD calculated from dose-response curves obtained from three independent experiments using cytotoxicity assay as described in Materials and methods.
‡ RF values were obtained by dividing IC50 values of ABCB1- or ABCG2- overexpressing cells by IC50 values of respective parental cells.
*
P < 0.05;
**
P < 0.01;
***
P < 0.001