Table 2 MDR reversal effect of FW-04-806 on ABCBl or ABCG2 non-substrate drugs
Compound | IC50 ± SD μM (fold-reversal) | Fold-resistance | |||
|---|---|---|---|---|---|
KB | KBv200(ABCB1) | ||||
Cisplatin | 3.8680 ± 1.3483 | (1.00) | 5.4893 ± 1.5035 | (1.00) | 1.4 |
 + 1.25 μM FW-04-806 | 2.0117 ± 0.1632 | (1.92) | 5.5650 ± 1.2172 | (0.99) |  |
 + 2.5 μM FW-04-806 | 3.7403 ± 0.5553 | (1.03) | 4.0650 ± 0.4293 | (1.35) |  |
 + 5 μM FW-04-806 | 2.2227 ± 0.3665 | (1.74) | 7.6887 ± 3.0405 | (0.71) |  |
 + 10 μM Verapamil | 1.8723 ± 0.3514 | (2.07) | 5.4337 ± 2.1716 | (1.01) |  |
| Â | K562 | K562/adr (ABCB1) | Â | ||
Cisplatin | 1.0181 ± 0.2686 | (1.00) | 5.8687 ± 0.7091 | (1.00) | 5.8 |
 + 1.25 μM FW-04-806 | 1.0200 ± 0.0362 | (1.00) | 7.1563 ± 1.4092 | (0.82) |  |
 + 2.5 μM FW-04-806 | 1.0510 ± 0.1333 | (0.97) | 7.7360 ± 0.5774 | (0.76) |  |
 + 5 μM FW-04-806 | 1.1273 ± 0.0605 | (0.90) | 6.4127 ± 0.9883 | (0.92) |  |
 + 10 μM Verapamil | 0.8974 ± 0.0791 | (1.13) | 6.0500 ± 1.6236 | (0.97) |  |
| Â | MCF-7 | MCF-7/adr (ABCB1) | Â | ||
Cisplatin | 15.0700 ± 0.3928 | (1.00) | 18.0167 ± 0.4153 | (1.00) | 1.2 |
 + 1.25 μM FW-04-806 | 18.7367 ± 0.1401 | (0.80) | 18.0933 ± 1.0193 | (1.00) |  |
 + 2.5 μM FW-04-806 | 13.7733 ± 0.5398 | (1.09) | 18.9100 ± 0.2905 | (0.95) |  |
 + 5 μM FW-04-806 | 16.4433 ± 0.4456 | (0.92) | 16.7633 ± 0.0981 | (1.07) |  |
 + 10 μM Verapamil | 18.4767 ± 1.1412 | (0.82) | 20.6867 ± 0.9530 | (0.87) |  |
| Â | HEK293/pcDNA3.1 | HEK293/ABCB1 | Â | ||
Cisplatin | 6.8007 ± 0.0765 | (1.00) | 8.6940 ± 0.1404 | (1.00) | 1.3 |
 + 2.5 μM FW-04-806 | 5.7683 ± 0.0093 | (1.18) | 9.2183 ± 0.2919 | (0.94) |  |
 + 5 μM FW-04-806 | 5.6213 ± 0.0837 | (1.21) | 7.5417 ± 0.2921 | (1.15) |  |
 + 10 μM FW-04-806 | 5.1467 ± 0.0979 | (1.32) | 7.7477 ± 0.0916 | (1.12) |  |
 + 10 μM Verapamil | 5.2640 ± 0.0900 | (1.29) | 7.3300 ± 0.2154 | (1.19) |  |
| Â | S1 | S1-MI-80(ABCG2) | Â | ||
Cisplatin | 12.7233 ± 0.5525 | (1.00) | 12.8800 ± 0.0608 | (1.00) | 1.01 |
 + 2.5 μM FW-04-806 | 12.9067 ± 0.4382 | (0.99) | 13.3100 ± 0.6678 | (0.97) |  |
 + 5 μM FW-04-806 | 15.1167 ± 0.3386 | (0.84) | 17.8867 ± 0.3785 | (0.72) |  |
 + 10 μM FW-04-806 | 13.2400 ± 0.1967 | (0.96) | 14.6533 ± 0.4388 | (0.88) |  |
 + 2.5 μM KO134 | 15.5033 ± 0.1124 | (0.82) | 16.2633 ± 0.2538 | (0.79) |  |
| Â | H460 | H460/MX20(ABCG2) | Â | ||
Cisplatin | 4.1593 ± 0.0618 | (1.00) | 15.9633 ± 0.3653 | (1.00) | 3.8 |
 + 2.5 μM FW-04-806 | 3.4410 ± 0.3634 | (1.21) | 15.8067 ± 0.5622 | (1.01) |  |
 + 5 μM FW-04-806 | 3.2287 ± 0.0302 | (1.29) | 17.2300 ± 0.2685 | (0.93) |  |
 + 10 μM FW-04-806 | 3.8967 ± 0.0093 | (1.07) | 14.8167 ± 0.2974 | (1.08) |  |
 + 2.5 μM KO134 | 4.0677 ± 0.1045 | (1.02) | 17.0767 ± 1.3276 | (0.93) |  |
| Â | HEK293/pcDNA3.1 | HEK293/ABCG2-R2 | Â | ||
Cisplatin | 6.8007 ± 0.0765 | (1.00) | 3.8733 ± 0.1240 | (1.00) | 0.57 |
 + 1.25 μM FW-04-806 | 6.1203 ± 0.0740 | (1.11) | 3.5323 ± 0.1928 | (1.10) |  |
 + 2.5 μM FW-04-806 | 6.0470 ± 0.0252 | (1.12) | 4.6223 ± 0.1293 | (0.84) |  |
 + 5 μM FW-04-806 | 6.4633 ± 0.2812 | (1.05) | 3.9990 ± 0.0717 | (0.97) |  |
 + 2.5 μM KO134 | 6.8980 ± 0.2655 | (0.99) | 4.7723 ± 0.4980 | (0.81) |  |