Table 1.

Effect of CM082 on Chemotherapeutic Agents in ABC Transporter-Expressing Cells In Vitro

Compounds	IC50 ± SD (μM) (Fold Reversal)
	KB		KBV200
DOX	0.0341 ± 0.0051	(1.00)	0.6153 ± 0.0678	(1.00)
+1.25 μM CM082	0.0364 ± 0.0019	(0.94)	0.6292 ± 0.0162	(0.98)
+2.5 μM CM082	0.0367 ± 0.0032	(0.93)	0.6031 ± 0.0523	(1.02)
+5 μM CM082	0.0339 ± 0.0031	(1.01)	0.6120 ± 0.0488	(1.01)
+10 μM VRP	0.0324 ± 0.0054	(1.05)	0.0983 ± 0.0067	(6.26)	**
DDP	0.4626 ± 0.0668	(1.00)	2.215 ± 0.2592	(1.00)
+5 μM CM082	0.5341 ± 0.0411	(0.87)	2.3753 ± 0.0421	(0.93)
	S1		S1-MI-80
MX	0.1669 ± 0.0205	(1.00)	3.9816 ± 0.1926	(1.00)
+1.25 μM CM082	0.1838 ± 0.0057	(0.91)	1.8476 ± 0.0819	(2.15)	**
+2.5 μM CM082	0.1561 ± 0.0289	(1.07)	0.9935 ± 0.0801	(4.01)	**
+5 μM CM082	0.1513 ± 0.0234	(1.10)	0.7887 ± 0.0371	(5.05)	**
+2.5 μM FTC	0.1570 ± 0.0161	(1.06)	0.5602 ± 0.0806	(7.11)	**
Topotecan	0.0701 ± 0.0067	(1.00)	12.593 ± 0.6403	(1.00)
+1.25 μM CM082	0.0783 ± 0.0078	(0.90)	5.264 ± 0.2486	(2.39)	**
+2.5 μM CM082	0.0740 ± 0.0071	(0.95)	3.1136 ± 0.5521	(4.04)	**
+5 μM CM082	0.0696 ± 0.0057	(1.01)	2.5146 ± 0.2676	(5.01)	**
+2.5 μM FTC	0.0725 ± 0.0078	(0.97)	0.7126 ± 0.0874	(17.67)	**
DDP	1.7123 ± 0.1378	(1.00)	3.9653 ± 0.5882	(1.00)
+5 μM CM082	1.777 ± 0.1294	(0.96)	4.1236 ± 0.4957	(0.96)
	H460		H460/MX20
MX	0.0226 ± 0.0008	(1.00)	0.6025 ± 0.0242	(1.00)
+1.25 μM CM082	0.0234 ± 0.0020	(0.97)	0.2924 ± 0.0361	(2.06)	**
+2.5 μM CM082	0.0243 ± 0.0020	(0.93)	0.2715 ± 0.0159	(2.22)	**
+5 μM CM082	0.0216 ± 0.0022	(1.04)	0.147 ± 0.0167	(4.10)	**
+2.5 μM FTC	0.0216 ± 0.0013	(1.04)	0.0928 ± 0.0047	(6.49)	**
DDP	2.4503 ± 0.4176	(1.00)	6.5106 ± 0.3045	(1.00)
+5 μM CM082	2.9673 ± 0.3366	(0.83)	6.268 ± 0.1615	(0.96)

An MTT assay was carried out to evaluate cell survival. VRP and FTC were employed as ABCB1- and ABCG2-positive control inhibitors, respectively. IC₅₀ values are shown as mean ± SD based on three separate experiments. By dividing the IC₅₀ of cells free from CM082 with the IC₅₀ of cells under CM082, we obtained the fold reversal of MDR. **p < 0.01.