Table 1.
NVP-CGM097 sensitized ABCB1-substrate-selected resistant cells to ABCB1 substrates.
| Treatment | IC50 ± SDa (RFb) (μM) | |||
|---|---|---|---|---|
| SW620 | SW620/Ad300 | KB-3-1 | KB-C2 | |
| Doxorubicin | 0.232 ± 0.034 (1.00) | 19.687 ± 0.711 (84.86) | 0.011 ± 0.001 (1.00) | 1.575 ± 0.477 (143.18) |
| +NVP CGM097 (1 μM) | 0.307 ± 0.033 (1.32) | 6.831 ± 1.030 (29.44)* | 0.011 ± 0.002 (1.00) | 0.344 ± 0.082 (31.27)* |
| +NVP CGM097 (3 μM) | 0.215 ± 0.018 (0.92) | 1.462 ± 0.212 (6.30)* | 0.012 ± 0.001 (1.09) | 0.047 ± 0.007 (4.27)* |
| +Verapamil (3 μM) | 0.222 ± 0.022 (0.95) | 1.511 ± 0.087 (6.51)* | 0.013 ± 0.001 (1.18) | 0.065 ± 0.027 (5.91)* |
| Paclitaxel | 0.220 ± 0.01 (1.00) | 20.95 ± 1.47 (95.22) | 0.016 ± 0.002 (1.00) | 1.897 ± 0.133 (118.56) |
| +NVP CGM097 (1 μM) | 0.196 ± 0.02 (0.89) | 3.453 ± 0.59 (15.70)* | 0.015 ± 0.002 (0.94) | 0.378 ± 0.129 (23.63)* |
| +NVP CGM097 (3 μM) | 0.237 ± 0.02 (1.08) | 0.843 ± 0.32 (3.83)* | 0.014 ± 0.001 (0.88) | 0.021 ± 0.018 (1.31)* |
| +Verapamil (3 μM) | 0.206 ± 0.07 (0.94) | 0.957 ± 0.12 (4.35)* | 0.015 ± 0.001 (0.94) | 0.032 ± 0.002 (2.00)* |
| Cisplatin | 1.021 ± 0.112 (1.00) | 1.109 ± 0.113 (1.09) | 1.259 ± 0.104 (1.00) | 1.091 ± 0.071 (0.87) |
| +NVP CGM097 (1 μM) | 1.093 ± 0.093 (1.07) | 1.237 ± 0.101 (1.21) | 1.206 ± 0.196 (0.96) | 1.173 ± 0.091 (0.93) |
| +NVP CGM097 (3 μM) | 1.236 ± 0.094 (1.21) | 1.117 ± 0.122 (1.09) | 1.096 ± 0.016 (0.87) | 1.242 ± 0.109 (0.99) |
| +Verapamil (3 μM) | 0.918 ± 0.098 (0.90) | 1.102 ± 0.093 (1.07) | 1.689 ± 0.078 (1.34) | 1.342 ± 0.137 (1.07) |
a
IC50 values were determined by MTT assay as described in “Materials and Methods,” and were obtained from three independent experiments in triplicate.
b
Resistance fold (RF) was calculated from dividing the IC50 values of resistant cells (SW620/Ad300 and KB-C2) by the IC50 of parental cells (SW620 and KB-3-1) in the presence or absence of NVP-CGM097 or positive control inhibitor.
*
p < 0.05 vs. group treated with antineoplastic drug only.