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. 2020 Jun 29;111(8):2872–2882. doi: 10.1111/cas.14505

TABLE 1.

Reversal effect of CC‐671 in non‐small cell lung cancer cells overexpressing ABCG2 transporter

Treatment IC50 value ± SD a (μmol/L, resistance‐fold b )
NCI‐H460 NCI‐H460/MX20 A549 A549/MX10
Mitoxantrone 0.011 ± 0.003 (1.00) 1.437 ± 0.326 (125.13) 0.026 ± 0.009 (1.00) 2.401 ± 0.486 (76.78)
+ CC‐671 0.1 μmol/L 0.014 ± 0.006 (1.20) 0.081 ± 0.006 (7.09)* 0.027 ± 0.004 (1.07) 0.633 ± 0.255 (20.24)*
+ CC‐671 0.3 μmol/L 0.013 ± 0.004 (1.16) 0.053 ± 0.004 (4.63)* 0.021 ± 0.005 (0.83) 0.252 ± 0.064 (8.06)*
+ CC‐671 1 μmol/L 0.012 ± 0.002 (1.07) 0.038 ± 0.002 (3.34)* 0.025 ± 0.008 (0.96) 0.144 ± 0.032 (4.61) *
+ Ko143 1 μmol/L 0.014 ± 0.007 (1.19) 0.044 ± 0.003 (3.87)* 0.028 ± 0.007 (1.10) 0.181 ± 0.040 (5.78) *
Topotecan 0.043 ± 0.025 (1.00) 3.003 ± 0.641 (69.12) 0.035 ± 0.003 (1.00) 1.401 ± 0.486 (40.03)
+ CC‐671 0.1 μmol/L 0.053 ± 0.008 (1.23) 0.504 ± 0.115 (11.61)* 0.033 ± 0.004 (0.94) 0.531 ± 0.147 (15.17) *
+ CC‐671 0.3 μmol/L 0.068 ± 0.024 (1.56) 0.411 ± 0.095 (9.46)* 0.032 ± 0.007 (0.92) 0.326 ± 0.034 (9.31) *
+ CC‐671 1 μmol/L 0.064 ± 0.018 (1.46) 0.242 ± 0.040 (5.58)* 0.041 ± 0.011 (1.17) 0.166 ± 0.029 (4.74) *
+ Ko143 1 μmol/L 0.059 ± 0.028 (1.37) 0.218 ± 0.088 (5.01)* 0.028 ± 0.004 (0.82) 0.210 ± 0.021 (6.06) *
Cisplatin 3.730 ± 0.834 (1.00) 5.198 ± 2.412 (1.39) 4.730 ± 0.534 (1.00) 3.991 ± 0.187 (0.84)
+ CC‐671 1 μmol/L 3.581 ± 0.388 (0.96) 5.106 ± 1.334 (1.37) 4.987 ± 0.561 (0.95) 4.847 ± 0.406 (1.02)
+ Ko143 1 μmol/L 3.067 ± 0.947 (0.82) 4.028 ± 0.581 (1.08) 4.991 ± 0.287 (1.06) 4.067 ± 0.347 (0.86)
a

IC50 values are represented as mean ± SD of at least 3 independent experiments carried out in triplicate.

b

Calculated by dividing the IC50 values of substrates in the presence or absence of inhibitor by the IC50 of parental cells without inhibitor.

*

P < .05 vs. control group without reversal agent.