Table 1.

Effect of nilotinib on reversing ABCB1-, ABCG2-, ABCC1- and ABCC4- mediated drug resistance.

Compounds	IC50 ± SD (μM) (Fold-Reversal)
	KB		KBv200 (ABCB1)
Doxorubicin	0.998 ± 0.013	(1.00)		18.51 ± 0337	(1.00)
+ 0.5 μM Nilotinib	0.874 ± 0.055	(1.14)		4.325 ± 0.047	(4.28) **
+ 1.0 μM Nilotinib	0.540 ± 0.014	(1.85) *		2.135 ± 0.065	(8.67) **
+ 2.0 μM Nilotinib	0.363 ± 0.006	(2.75) *		0.876 ± 0.075	(21.1) **
+ 10 μM Verapamil	0.629 ± 0.008	(1.57)		1.351 ± 0.036	(13.7) **
Daunorubicin	0.493 ± 0.42	(1.00)		17.33 ± 0.044	(1.00)
+ 0.5 μM Nilotinib	0.312 ± 0.020	(1.58)		5.252 ± 0.135	(3.30) **
+ 1.0 μM Nilotinib	0.298 ± 0.084	(1.65) *		3.365 ± 0.097	(5.15) **
+ 2.0 μM Nilotinib	0.215 ± 0.039	(2.29) *		1.223 ± 0.086	(14.2) **
+ 10 μM Verapamil	0.351 ± 0.068	(1.40)		0.873 ± 0.078	(19.9) **
Cisplatin	1.682 ± 0.073	(1.00)		2.632 ± 0.261	(1.00)
+ 2.0 μM Nilotinib	1.567 ± 0.142	(0.93)		2.346 ± 0.218	(0.89)
	S1			S1-M1-80 (ABCG2)
Mitoxantrone	0.310 ± 0.031	(1.00)		23.60 ± 0.980	(1.00)
+ 0.5 μM Nilotinib	0.286 ± 0.074	(1.08)		5.626 ± 0.035	(4.19) **
+ 1.0 μM Nilotinib	0.245 ± 0.041	(1.26)		1.405 ± 0.039	(16.8) **
+ 2.0 μM Nilotinib	0.243 ± 0.036	(1.28)		0.590 ± 0.052	(40.0) **
+ 2.5 μM FTC	0.238 ± 0.013	(1.30)		0.289 ± 0.023	(81.7) **
Topotecan	0.365 ± 4.381	(1.00)		25.43 ± 5.442	(1.00)
+ 0.5 μM Nilotinib	0.297 ± 0.063	(1.23)		7.27 ± 0.141	(3.50) **
+ 1.0 μM Nilotinib	0.287 ± 0.034	(1.27)		4.19 ± 0.451	(6.07) **
+ 2.0 μM Nilotinib	0.208 ± 0.019	(1.75)		1.78 ± 0.372	(14.3) **
+ 2.5 μM FTC	0.245 ± 0.032	(1.49)		0.48 ± 0.012	(53.0) **
Cisplatin	14.788 ±1.678	(1.00)		16.428 ± 1.851	(1.00)
+ 2.0 μM Nilotinib	14.118±1.335	(0.95)		15.390 ± 1.356	(0.94)
	HL60			HL60/ADR (ABCC1)
Doxorubicin	0.059 ± 0.009	(1.00)		1.191 ± 0.074	(1.00)
+ 0.5 μM Nilotinib	0.069 ± 0.002	(0.86)		1.009 ± 0.032	(1.18)
+ 1.0 μM Nilotinib	0.040 ± 0.006	(1.48)		0.775 ± 0.074	(1.54)
+ 2.0 μM Nilotinib	0.058 ± 0.016	(1.02)		0.862 ± 0.076	(1.38)
+ 50 μM MK571	0.039 ± 0.003	(1.51)		0.069 ± 0.007	(17.3) **
	NIH3T3			NIH3T3/MRP4 (ABCC4)
6-Mercaptopurine	0.029 ± 0.002	(1.00)		0.32 ± 0.005	(1.00)
+ 0.5 μM Nilotinib	0.025 ± 0.004	(1.16)		0.30 ± 0.002	(1.06)
+ 1.0 μM Nilotinib	0.030 ± 0.001	(0.98)		0.31 ± 0.001	(1.03)
+ 2.0 μM Nilotinib	0.028 ± 0.003	(1.04)		0.24 ± 0.003	(1.33)

Cell survival was determined by MTT. Data are the mean ± standard deviations (SDs) of at least three independent experiments performed in triplicate. The fold reversal of MDR was calculated by dividing the IC₅₀ value for cells with the anticancer drug in the absence of nilotinib by that obtained in the presence of nilotinib. * p < 0.05; ** p < 0.01.