Table 1. Icotinib reverse the ABCG2-mediated drug resistance in drug selected resistant NSCLC cells.
IC50 ± SDa (μM) | ||||||
---|---|---|---|---|---|---|
Compounds | A549 | (RF)b | NCI-H460 | (RF)b | NCI-H460/MX20 | (RF)b |
Mitoxantrone (μM) | 0.2853 ± 0.0214 | 1 | 0.0668 ± 0.0033 | 1.0 | 5.0837 ± 0.7542 | 76.0 |
+ Icotinib 1.0 μM | 0.2269 ± 0.0193 | 0.8 | 0.0354 ± 0.0028* | 0.5 | 1.9336 ± 0.1121* | 28.9 |
+ Icotinib 5.0 μM | 0.1695 ± 0.0102* | 0.6 | 0.0314 ± 0.0022* | 0.5 | 0.3559 ± 0.0249* | 5.3 |
+ FTC 5.0 μM | 0.1858 ± 0.0167* | 0.7 | 0.0300 ± 0.0023* | 0.4 | 0.3316 ± 0.0265* | 5.0 |
SN-38 (μM) |
0.6251 ± 0.0313 | 1.0 | 0.0707 ± 0.0035 | 1.0 | 8.1222 ± 1.006 | 114.9 |
+ Icotinib 1.0 μM | 0.2482 ± 0.0199* | 0.4 | 0.0202 ± 0.0016* | 0.3 | 2.6770 ± 0.1553* | 37.8 |
+ Icotinib 5.0 μM | 0.1717 ± 0.0120* | 0.3 | 0.0150 ± 0.0011* | 0.2 | 0.3271 ± 0.0229* | 4.6 |
+ FTC 5.0 μM | 0.1752 ± 0.0131* | 0.3 | 0.0166 ± 0.0012* | 0.2 | 0.3126 ± 0.0250* | 4.4 |
Topotecan (μM) |
1.4551 ± 0.1237 | 1.0 | 0.0490 ± 0.0042 | 1.0 | 4.8721 ± 0.4141 | 99.4 |
+ Icotinib 1.0 μM | 0.9458 ± 0.0851* | 0.7 | 0.0226 ± 0.0020* | 0.5 | 0.1261 ± 0.0113* | 2.6 |
+ Icotinib 5.0 μM | 0.9313 ± 0.0931* | 0.6 | 0.0196 ± 0.0019* | 0.4 | 0.0598 ± 0.0060* | 1.2 |
+ FTC 5.0 μM | 1.0186 ± 0.0866* | 0.7 | 0.0194 ± 0.0016* | 0.4 | 0.0639 ± 0.0054* | 1.3 |
Cisplatin (μM) |
2.7677 ± 0.2214 | 1.0 | 1.2692 ± 0.1015 | 1.0 | 1.3200 ± 0.1056 | 1.0 |
+ Icotinib 5.0 μM | 2.9831 ± 0.1492 | 1.1 | 1.2727 ± 0.0636 | 1.0 | 1.2012 ± 0.0841 | 0.9 |
+ FTC 5.0 μM | 3.2343 ± 0.2264 | 1.2 | 1.2017 ± 0.0841 | 0.9 | 1.2540 ± 0.0627 | 1.0 |
IC50 values are represented the mean ± standard deviation (SD).
Resistance fold (RF) was calculated by the IC50 values for different substrates, and cisplatin of NCI-H460/MX20 cells, divided by the IC50 values for the respective control without the reversing agents, or the resistant cell lines in the presence or absence of Icotinib or FTC, divided by the IC50 values for different substrates, and cisplatin of respective control without the reversing agents.
. P < 0.05, versus the control group