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Table 1 Effect of axitinib on reversing ABCG2-mediated drug resistance.a

From: Axitinib Targeted Cancer Stemlike Cells to Enhance Efficacy of Chemotherapeutic Drugs via Inhibiting the Drug Transport Function of ABCG2

Compounds IC50 ± SD, µmol/L (Fold reversal)
S1 S1-M1-80(ABCG2)
Topetecan 0.250 ± 0.014 (1.00) 12.79 ± 0.241 (1.00)
+0.25 µmol/L Axitinib 0.249 ± 0.020 (1.01) 6.692 ± 0.504b (1.85)
+0.5 µmol/L Axitinib 0.255 ± 0.017 (0.98) 4.964 ± 0.320b (2.47)
+ 1.0 µmol/L Axitinib 0.199 ± 0.006 (1.26) 3.020 ± 0.242b (4.11)
+0.5 µmol/L FTC 0.244 ± 0.013 (1.02) 1.195 ± 0.108b (10.7)
Mitoxantrone 0.193 ± 0.021 (1.00) 14.668 ± 0.636 (1.00)
+0.25 µmol/L Axitinib 0.194 ± 0.057 (0.99) 7.992 ± 0.675b (1.84)
+0.5 µmol/L Axitinib 0.201 ± 0.011 (0.96) 4.140 ± 0.301b (3.54)
+ 1.0 µmol/L Axitinib 0.185 ± 0.011 (1.12) 2.904 ± 0.482b (5.05)
+0.5 µmol/L FTC 0.188 ± 0.011 (1.03) 1.272 ± 0.056b (11.5)
Cisplatin 14.877 ± 1.126 (1.00) 14.496 ± 1.112 (1.00)
+ 1.0 µmol/L Axitinib 14.206 ± 1.460 (1.05) 14.360 ± 1.812 (1.01)
  KB KBv200(ABCB1)
Doxorubicin 0.024 ± 0.002 (1.00) 2.204 ± 0.108 (1.00)
+0.25 µmol/L Axitinib 0.024 ± 0.002 (1.00) 2.022 ± 0.185 (1.08)
+0.5 µmol/L Axitinib 0.025 ± 0.001 (0.96) 2.153 ± 0.146 (1.02)
+ 1.0 µmol/L Axitinib 0.015 ± 0.004c (1.63) 1.250 ± 0.215c (1.76)
+ 10 µmol/L Verapamil 0.024 ± 0.003 (1.00) 0.109 ± 0.008b (20.2)
Cispatin 1.552 ± 0.121 (1.00) 2.364 ± 0.241 (1.00)
+ 1.0 µmol/L Axitinib 1.514 ± 0.117 (1.03) 2.412 ± 0.225 (0.98)
  HL60 HL60/ADR(ABCC1)
Doxorubicin 0.055 ± 0.011 (1.00) 5.725 ± 0.203 (1.00)
+0.1 µmol/L Axitinib 0.054 ± 0.006 (1.02) 5.719 ± 0.591 (1.00)
+0.2 µmol/L Axitinib 0.056 ± 0.006 (0.98) 5.759 ± 0.659 (0.99)
+0.4 µmol/L Axitinib 0.049 ± 0.005 (1.13) 5.476 ± 0.384 (1.04)
+40 µmol/L MK571 0.054 ± 0.005 (1.02) 1.108 ± 0.182b (5.17)
Cisplatin 1.456 ± 0.187 (1.00) 1.658 ± 0.118 (1.00)
+0.4 µmol/L Axitinib 1.516 ± 0.125 (0.96) 1.524 ± 0.175 (1.08)
  SW1573 SW1573/2R120(LRP)
Doxorubicin 0.108 ± 0.012 (1.00) 1.266 ± 0.121 (1.00)
+0.25 µmol/L Axitinib 0.096 ± 0.004 (1.12) 1.214 ± 0.174 (1.04)
+0.5 µmol/L Axitinib 0.098 ± 0.004 (1.10) 1.236 ± 0.122 (1.02)
+ 1.0 µmol/L Axitinib 0.094 ± 0.006 (1.14) 1.138 ± 0.088 (1.11)
Cisplatin 2.473 ± 0.167 (1.00) 9.659 ± 1.073 (1.00)
+ 1.0 µmol/L Axitinib 2.790 ± 0.147 (0.89) 9.180 ± 0.881 (1.05)
  NIH3T3 NIH3T3/MRP4-2(ABCC4)
6-MP 0.298 ± 0.050 (1.00) 11.852 ± 1.564 (1.00)
+0.25 µmol/L Axitinib 0.285 ± 0.034 (1.04) 11.145 ± 1.048 (1.06)
+0.5 µmol/L Axitinib 0.318 ± 0.045 (0.94) 10.709 ± 1.637 (1.11)
+ 1.0 µmol/L Axitinib 0.265 ± 0.011 (1.12) 12.319 ± 1.704 (0.96)
Cisplatin 6.140 ± 0.728 (1.00) 5.668 ± 0.690 (1.00)
+ 1.0 µmol/L Axitinib 5.033 ± 0.296 (1.21) 5.842 ± 0.691 (0.97)
  1. aCell survival was determined by MTT assays as described in Materials and Methods. Data are the mean ± standard deviation (SD) of at least three independent experiments performed in triplicate. The fold reversal of MDR (values given in parentheses) was calculated by dividing the IC50 for cells with the anticancer drugs in the absence of axitinib by that obtained in the presence of axitinib. bP < 0.01; cP < 0.05 versus the values obtained in the absence of inhibitor