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

TABLE 2.

Reversal effect of CC‐671 in HEK293 transfected cells overexpressing ABCG2 transporter

Treatment	IC₅₀ value ± SD ^a (μmol/L, resistance‐fold ^b )
Treatment	pcDNA3.1	ABCG2‐WT	ABCG2‐R482G	ABCG2‐R482T
Mitoxantrone	0.018 ± 0.002 (1.00)	0.590 ± 0.102 (32.42)	0.417 ± 0.147 (22.95)	1.342 ± 0.263 (73.81)
+ CC‐671 0.1 μmol/L	0.022 ± 0.006 (1.05)	0.179 ± 0.026 (9.85)^*	0.111 ± 0.042 (6.11)^*	0.545 ± 0.321 (29.98)^*
+ CC‐671 0.3 μmol/L	0.024 ± 0.004 (1.13)	0.035 ± 0.014 (1.92)^*	0.035 ± 0.018 (1.92)^*	0.124 ± 0.036 (6.85) ^*
+ Ko143 0.3 μmol/L	0.020 ± 0.009 (0.79)	0.022 ± 0.012 (1.22)^*	0.032 ± 0.005 (1.75)^*	0.021 ± 0.008 (1.15) ^*
Topotecan	0.104 ± 0.030 (1.00)	2.628 ± 1.319 (25.30)	4.856 ± 1.482 (46.73)	6.107 ± 0.656 (58.77)
+ CC‐671 0.1 μmol/L	0.121 ± 0.036 (1.16)	0.706 ± 0.228 (6.79)^*	0.977 ± 0.348 (9.40)^*	2.971 ± 0.131 (28.59)^*
+ CC‐671 0.3 μmol/L	0.155 ± 0.064 (1.49)	0.466 ± 0.067 (4.48)^*	0.343 ± 0.170 (3.30)^*	0.277 ± 0.090 (2.67) ^*
+ Ko143 0.3 μmol/L	0.124 ± 0.040 (1.19)	0.275 ± 0.140 (2.64)^*	0.130 ± 0.019 (1.26)^*	0.332 ± 0.125 (3.20) ^*
Cisplatin	8.247 ± 1.125 (1.00)	12.853 ± 0.083 (1.56)	7.605 ± 1.288 (0.92)	7.895 ± 0.795 (0.95)
+ CC‐671 0.3 μmol/L	8.759 ± 3.243 (1.06)	11.564 ± 2.415 (1.40)	11.752 ± 2.171 (1.43)	9.351 ± 1.636 (1.13)
+ Ko143 0.3 μmol/L	6.234 ± 0.137 (0.76)	11.758 ± 2.923 (1.43)	10.050 ± 2.756 (1.22)	7.325 ± 1.124 (0.89)

^{^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.