. Author manuscript; available in PMC: 2015 Aug 1.

Published in final edited form as: J Cell Biochem. 2014 Aug;115(8):1381–1391. doi: 10.1002/jcb.24787

Table 1.

ARRY-334543 reverse the ABCG2-mediated drug resistance in drug selected resistant cells.

	IC₅₀ ± SD^a (μM)
Compounds	NCI-H460	(RF)^b	NCI-H460/MX20	(RF)^b
Mitoxantrone (μM)	0.0608 ± 0.0043	1.0	5.0173 ± 1.2616	82.5
+ARRY-334543 0.25 μM	0.0289 ± 0.0023^*	0.5	1.5613 ± 0.1093^*	25.7
+ARRY-334543 1.0 μM	0.0272 ± 0.0025^*	0.4	0.3257 ± 0.0261^*	5.4
+ FTC 5.0 μM	0.0243 ± 0.0019^*	0.4	0.3177 ± 0.0222^*	5.2
SN-38 (μM)	0.0649 ± 0.0052	1.0	8.9194 ± 1.5135	137.4
+ARRY-334543 0.25 μM	0.0166 ± 0.0012^*	0.3	2.0939 ± 0.1570^*	32.3
+ARRY-334543 1.0 μM	0.0153 ± 0.0013^*	0.2	0.3825 ± 0.0325^*	5.9
+ FTC 5.0 μM	0.0151 ± 0.0012^*	0.2	0.3773 ± 0.0211^*	5.8
Cisplatin (μM)	1.1977 ± 0.0958	1.0	1.2152 ± 0.0608	1.0
+ARRY-334543 0.25 μM	1.2632 ± 0.0884	1.1	1.1638 ± 0.0815	1.0
+ARRY-334543 1.0 μM	1.2761 ± 0.0893	1.1	1.1774 ± 0.0706	1.0
+ FTC 5.0 μM	1.2392 ± 0.0867	1.0	1.1376 ± 0.0830	0.9

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 cell with either ARRY-334543 or Fumitremorgin C (FTC), or the NCI-H460/MX20 cell in the presence or absence of ARRY-334543 or FTC, divided by the IC₅₀ values for different substrates, and cisplatin of NCI-H460 cell without the reversing agents.

P < 0.05, versus the control group.