Table 1.
Cytotoxicity of SKLB610 in human cell lines overexpressing ABCB1 or ABCG2.
| Cell line | Type | Transporter overexpressed |
IC50 (μM)a | RFb |
|---|---|---|---|---|
|
| ||||
| KB-3–1 | Epidermal | – | 15.75 ± 2.48 | 1.0 |
| KB-V1 | Epidermal | ABCB1 | 10.75 ± 2.32 | 0.7 |
| OVCAR-8 | Ovarian | – | 20.92 ± 1.31 | 1.0 |
| NCI-ADR-RES | Ovarian | ABCB1 | 25.07 ± 2.64 | 1.2 |
| H460 | Lung | – | 31.07 ± 3.22 | 1.0 |
| H460-MX20 | Lung | ABCG2 | 25.10 ± 2.76 | 0.8 |
| S1 | Colon | – | 16.06 ± 4.15 | 1.0 |
| S1-MI-80 | Colon | ABCG2 | 17.06 ± 2.26 | 1.1 |
| pcDNA3.1-HEK293 | – | – | 54.72 ± 7.46 | 1.0 |
| MDR19-HEK293 | – | ABCB1 | 68.61 ± 12.58 | 1.3 |
| R482-HEK293 | – | ABCG2 | 77.76 ± 12.89 | 1.4 |
Abbreviations: RF, resistance factor.
IC50 values were calculated from dose-response curves obtained from at least three independent experiments as described in Section 2.
RF values were obtained by dividing the IC50 value of SKLB610 in the ABCB1- or ABCG2-overexpressing multidrug-resistant cell lines by the IC50 value of SKLB610 in the corresponding drug-sensitive parental cell lines.