Drug | Mock-HEK | OCT2-HEK | MATE1-HEK | MATE2K-HEK | |||
---|---|---|---|---|---|---|---|
IC50(CN) | IC50(CN) | RFa | IC50(CN) | RFa | IC50(CN) | RFa | |
Cisplatin only | 2.34 ± 0.31 | 1.36 ± 0.19 | 1.7 | 1.12 ± 0.13 | 2.1 | 0.85 ± 0.09b | 2.8 |
Cisplatin + vandetanib (2.5 µM) | 2.31 ± 0.31 | 1.47 ± 0.24 | 1.6 | 2.39 ± 0.44c | 1.0 | 1.99 ± 0.16c | 1.2 |
Cisplatin + PYR (2.5 µM) | ND | ND | – | 2.28 ± 0.19 | 1.1 | 2.23 ± 0.28c | 1.1 |
Cisplatin + PYR (50 µM) | 2.39 ± 0.42 | 2.38 ± 0.31 | 1.0 | ND | – | ND | – |
↵ND, not determined; RF, resistance factor.aIC50(CN) after addition of cisplatin to HEK293 cells stably transfected with transporter versus the IC50(CN) after addition of cisplatin to vector only (mock) transfected HEK293 cells; PYR, pyrimethamine.
↵b Statistically significant left shift in IC50(CN) versus cisplatin alone in mock-HEK cells (P < 0.05).
↵c For MATE1-HEK and MATE2K-HEK cells, there was a statistically significant right shift in IC50(CN) versus cisplatin alone in MATE1-HEK and MATE2K-HEK (P < 0.05).