Table 1.

Effects of the test compounds in reversing ABCG2-mediated resistance to mitoxantrone

Treatment		HEK293/pcDNA3.1				ABCG2-482-R2
		IC50(nM)			FR a	IC50(nM)			FR a
Mitoxantrone		17.77	±	1.34	1.00	227.40	±	14.95	12.80
+OSI-930	10 µM	23.17	±	3.37	1.30	42.24	±	17.56	2.38
+VKJP1	10 µM	11.28	±	1.23	0.63	14.90	±	8.70	0.84
+VKJP2	10 µM	18.95	±	7.45	1.07	61.81	±	14.77	3.48
+VKJP3	10 µM	10.68	±	0.84	0.60	35.15	±	11.96	1.98
+VKJP4	10 µM	17.24	±	2.96	0.97	58.95	±	0.94	3.32
+VKJP5	10 µM	14.93	±	0.92	0.84	50.59	±	5.57	2.85
+VKJP6	10 µM	20.42	±	0.69	1.15	61.88	±	9.23	3.48
+VKJP7	10 µM	15.64	±	4.01	0.88	67.21	±	11.78	3.78
+VKJP8	10 µM	16.40	±	3.35	0.92	79.48	±	20.81	4.47
+VKJP9	10 µM	18.32	±	8.31	1.03	54.82	±	24.55	3.08
+VKJP10	10 µM	17.35	±	8.45	0.98	53.93	±	25.04	3.03
+VKJP11	10 µM	15.72	±	1.94	0.88	65.34	±	25.35	3.68
+VKJP12	10 µM	22.36	±	6.90	1.26	54.66	±	17.06	3.08
+VKJP13	10 µM	17.96	±	1.40	1.01	217.52	±	18.65	12.20
+VKJP14	10 µM	19.97	±	5.74	1.12	257.63	±	35.88	14.50
+VKJP15	10 µM	14.51	±	2.49	0.82	57.05	±	26.69	3.21
+FTC	2.5 µM	16.15	±	1.19	0.91	20.17	±	2.38	1.14

^aFold-resistance was determined by dividing the IC₅₀ value for mitoxantrone of ABCG2-482-R2 cells by IC₅₀ value of HEK293/pcDNA3.1 cells in the absence or presence of the test compounds or FTC.