Table 1.
Sensitivity of drug-sensitive and multidrug-resistant cells overexpressing ABCB1 or ABCG2 to TP-3654.
| Cell Line | Type | Transporter Expressed | IC50 (μM) † |
|---|---|---|---|
| KB-3-1 | Epidermal | - | 19.07 ± 1.59 |
| KB-V-1 | Epidermal | ABCB1 | 24.50 ± 3.24 |
| OVCAR-8 | Ovarian | - | 34.33 ± 5.92 |
| NCI-ADR-RES | Ovarian | ABCB1 | 28.00 ± 3.38 |
| S1 | Colon | - | 4.10 ± 1.17 |
| S1-M1-80 | Colon | ABCG2 | 3.39 ± 0.39 |
| H460 | Lung | - | 22.26 ± 3.35 |
| H460-MX20 | Lung | ABCG2 | 22.05 ± 3.87 |
| pcDNA3.1-HEK293 | - | - | 2.76 ± 0.79 |
| MDR19-HEK293 | - | ABCB1 | 3.03 ± 0.59 |
| R482-HEK293 | - | ABCG2 | 2.55 ± 0.53 |
† IC50 values are mean ± SD calculated from dose–response curves obtained from at least three independent experiments using cytotoxicity assay as described in Section 4.