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. 2014 Jun 13;5(12):4529–4542. doi: 10.18632/oncotarget.2102

Table 2. The reversal efficacy of Icotinib in ABCG2-mediated drug resistance in ABCG2-transfected cell lines.

IC50 ± SDa (μM)
Compounds HEK293/pcDNA3.1 (RF)b ABCG2-482-R2 (RF)b ABCG2-482-G2 (RF)b ABCG2-482-T7 (RF)b
Mitoxantrone (μM) 0.0557 ± 0.0028 1.0 0.5754 ± 0.0460 10.3 1.7045 ± 0.1364 30.6 1.1045 ± 0.0884 19.8
+ Icotinib 1.0 μM 0.0533 ± 0.0037 1.0 0.3438 ± 0.0309* 6.2 0.7934 ± 0.0714* 14.3 0.5524 ± 0.0497* 9.9
+ Icotinib 5.0 μM 0.0503 ± 0.0040 0.9 0.0537 ± 0.0027* 1.0 0.0701 ± 0.0035* 1.3 0.0687 ± 0.0034* 1.2
+ FTC 5.0 μM 0.0491 ± 0.0022 0.9 0.0564 ± 0.0023* 1.0 0.0645 ± 0.0026* 1.2 0.0632 ± 0.0025* 1.1
SN-38 (μM) 0.0070 ± 0.00035 1.0 0.1885 ± 0.0151 27.1 0.2494 ± 0.0200 35.8 0.2095 ± 0.0168 30.1
+ Icotinib 1.0 μM 0.0067 ± 0.0005 1.0 0.0612 ±
0.0055*
8.8 0.0811 ± 0.0073* 11.7 0.0750 ± 0.0068* 10.8
+ Icotinib 5.0 μM 0.0063 ± 0.0005 0.9 0.0087 ± 0.0004* 1.2 0.0080 ± 0.0004*
1.2
0.0077 ± 0.0005* 1.1
+ FTC 5.0 μM 0.0061 ± 0.0003 0.9 0.0075 ± 0.0003* 1.1 0.0078 ± 0.0003* 1.1 0.0078 ± 0.0003* 1.1
Cisplatin (μM) 1.6700 ± 0.0835 1.0 1.7045 ± 0.1364 1.0 1.6045 ± 0.1284 1.0 1.6704 ± 0.1336 1.0
+ Icotinib 5.0 μM 1.5980 ± 0.1119 1.0 1.6662 ± 0.1500 1.0 1.5524 ± 0.1397 0.9 1.5500 ± 0.0775 0.9
+ FTC 5.0 μM 1.5098 ± 0.1208 0.9 1.5801 ± 0.0790 0.9 1.6873 ± 0.0844 1.0 1.5400 ± 0.1001 0.9
a.

IC50 values are represented the mean ± standard deviation (SD).

b.

Resistance fold (RF) was calculated by the IC50 values for different substrates, and cisplatin of resistant cell lines, 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.