IC50 | Resistance Factor | |||
---|---|---|---|---|
HEK293 | HEK293/5I (MRP5) | HEK293/4.3 (MRP4) | HEK293/4.63 (MRP4) | |
μM | ||||
Antiviral drugs | ||||
PMEDAP | 64 ± 3 (4) | 1.7 ± 0.2 (3) | 4.8 ± 0.7 (3) | 9.6 ± 0.9 (4) |
cPr-PMEDAP | 2 ± 0.2 (6) | 1.4 ± 0.1 (4) | 9.6 ± 1.1 (4) | 16.6 ± 2.1 (5) |
PMEG | 1.5 ± 0.1 (4) | 1.2 ± 0.2 (3) | 2.4 ± 0.3 (4) | 3.5 ± 0.3 (3) |
PMEA1-a | 84.1 ± 15 (6) | 2.9 ± 0.3 (10) | 3.6 ± 0.3 (6) | 7.3 ± 0.2 (2) |
bis-POM-PMEA1-a | 1.7 ± 0.5 (6) | 3.4 ± 0.5 (4) | 3.3 ± 0.2 (6) | 8.5 ± 0.1 (2) |
(S)-HPMPC | 136 ± 80 (2) | 1.2 ± 0.5 (2) | 1.2 ± 0.5 (2) | 1.2 ± 0.5 (2) |
Abacavir | 244 ± 86 (4) | 1.9 ± 0.4 (4)1-b | 2 ± 0.2 (4) | 2 ± 0.2 (3) |
Anticancer drugs | ||||
Cladribine | 2.0 ± 0.4 (6) | 1.5 ± 0.3 (4) | 1.7 ± 0.3 (5) | 2.2 ± 0.4 (3) |
Gemcitabine | 0.04 (5) | 1.0 ± 0.2 (3) | 1.1 ± 0.1 (5) | 1 ± 0.1 (4) |
Cytarabine | 1.1 ± 0.3 (5) | 1.0 ± 0.2 (5) | 1.3 ± 0.3 (5) | 1.2 ± 0.3 (5) |
Fludarabine | 67 ± 10 (4) | 1.1 ± 0.2 (4) | 1.1 ± 0.2 (4) | 1.3 ± 0.4 (2) |
5-Fluorouracil | 18 ± 2 (2) | 1 ± 0.2 (2) | 1 ± 0.2 (2) | 1.2 (1) |
Thioguanine1-a | 1 ± 0.2 (4) | 2.7 ± 0.1 (2) | 2.9 ± 0.6 (3) | 4.1 ± 0.1 (3) |
6-Mercaptopurine1-a | 5.2 ± 0.9 (4) | 3.0 ± 0.3 (4) | 2.7 ± 0.4 (3) | 5.6 ± 2.4 (3) |
No cytotoxicity was observed with So324, azidothymidine, d4T, 2′,3′-dideoxyadenosine, ddC, or 2′,3′-dideoxyinosine. Drugs were tested over a concentration range corresponding to at least 16-fold higher and lower than the IC50. The values in parentheses are the number of determinations