Table 1. Effect of AG1478, verapamil and valspodar on ABCB1-mediated resistance to colchicine, vinblastine, paclitaxel and cisplatin.a.
Compounds |
IC50 ± SD (μM) |
|
---|---|---|
KB-3-1 |
KB-C2 |
|
Colchicine | 0.0069±0.0010(1.0)a | 6.9543±0.2437(947.8) |
+ AG1478 10 μM | 0.0069±0.0004(1.0) | 3.6490±0.2268(505.8) |
+ Verapamil 10 μM | 0.0060±0.0003(0.9) | 0.1077±0.0134(15.6) |
0.0059±0.0007(0.9) | 0.0097±0.0056(1.41) | |
+ Valspodar 5 μM |
|
|
Vinblastine | 0.0476±0.0043(1.0)a | 0.3057±0.0152(6.4) |
+ AG1478 10 μM | 0.0428±0.0008(0.9) | 0.1644±0.0245(3.5) |
+ Verapamil 10 μM | 0.0408±0.0062(0.9) | 0.0419±0.0078(0.9) |
0.0389±0.0045(0.8) | 0.0399±0.0098(0.8) | |
+ Valspodar 5 μM |
|
|
Paclitaxel | 0.0084±0.0023(1.0)a | 5.5643±1.1098(662.3) |
+ AG1478 10 μM | 0.0079±0.0004(1.0) | 1.4461±0.2839(172.1) |
+ Verapamil 10 μM | 0.0072±0.0018(0.9) | 0.0173±0.0077(2.0) |
0.0068±0.0021(0.8) | 0.0093±0.0064(1.1) | |
+ Valspodar 5 μM |
|
|
Cisplatin | 1.8867±0.0446(1.0)a | 1.8235±0.0782(1.0) |
+ AG1478 10 μM | 1.8365±0.0578(1.0) | 1.8293±0.0811(1.0) |
+ Verapamil 10 μM | 1.8116±0.0824(1.0) | 1.7244±0.0387(0.9) |
1.8233±0.0718(1.0) | 1.8401±0.0702(1.0) | |
+ Valspodar 5 μM |
Fold-resistance was determined by dividing the IC50 values of KB-C2 cells by the IC50 values for KB-3-1 cells in the absence or presence of AG1478, verapamil or valspodar.