Table 1.
Cytotoxicity of ricolinostat in human cancer cell lines overexpressing ABCB1 or ABCG2.
| Cell line | Type | Transporter expressed | IC50 (μM)† | R.F‡ |
|---|---|---|---|---|
| KB-3–1 | epidermal | – | 4.28 ± 0.71 | 1.0 |
| KB-V-1 | epidermal | ABCB1 | 24.18 ± 2.05*** | 5.6 |
| OVCAR-8 | ovarian | – | 6.02 ± 0.91 | 1.0 |
| NCI-ADR-RES | ovarian | ABCB1 | 59.78 ± 7.98*** | 9.9 |
| S1 | colon | – | 3.06 ± 0.21 | 1.0 |
| S1-M1–80 | colon | ABCG2 | 69.01 ± 5.79*** | 22.6 |
| MCF7 | breast | – | 16.22 ± 3.58 | 1.0 |
| MCF7-FLV1000 | breast | ABCG2 | > 100 | > 6 |
| MCF7-AdVp3000 | breast | ABCG2 | > 100 | > 6 |
| NIH3T3 | – | – | 3.46 ± 0.70 | 1.0 |
| NIH3T3-G185 | – | ABCB1 | 32.57 ± 2.33*** | 9.4 |
| pcDNA-HEK293 | – | – | 3.40 ± 0.50 | 1.0 |
| MDR19-HEK293 | – | ABCB1 | 22.35 ± 2.05*** | 6.6 |
| R482-HEK293 | – | ABCG2 | 40.25 ± 4.36*** | 11.8 |
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 calculated by dividing IC50 values of ABC transporter overexpressing cells by IC50 values of respective parental cells.
*
P < 0.05;
**
P < 0.01;
***
P < 0.001.