Table 1 Effect of dacomitinib on enhancement of conventional chemotherapeutic agents
Compounds | IC50±SD (μM) (fold-reversal) | |
|---|---|---|
KB | KBV200(ABCB1) | |
DOX | 0.0620±0.0030 (1.00) | 0.4693±0.0299 (1.00) |
+0.25μM Dacomitinb | 0.0603±0.0114 (1.03) | 0.3720±0.0176 (1.26) |
+0.5μM Dacomitinb | 0.0591±0.0121 (1.05) | 0.3994±0.0865 (1.17) |
+1μM Dacomitinb | 0.0545±0.0102 (1.14) | 0.2950±0.4790 (1.59) |
+10μM VRP | 0.0540±0.0141 (1.15) | 0.0303±0.0180 (9.70)** |
DDP | 0.4477±0.0926 (1.00) | 0.8727±0.0385 (1.00) |
+1μM Dacomitinb | 0.4958±0.0525 (0.90 ) | 0.9865±0.8774 (0.88) |
H460 | H460/MX20(ABCG2) | |
MX | 0.0254±0.0068 (1.00) | 2.4569±0.0504 (1.00) |
+0.25μM Dacomitinb | 0.0309±0.0081 (0.82) | 0.6534±0.0803 (3.76)** |
+0.5μM Dacomitinb | 0.0162±0.0104 (1.50) | 0.1937±0.0105 (12.68)** |
+1μM Dacomitinb | 0.1529±0.0018 (1.12) | 0.1892±0.0073 (12.98)** |
+2.5μM FTC | 0.1921±0.0011 (1.30) | 0.3012±0.0233 (8.15)** |
DDP | 3.6240±0.8351 (1.00) | 9.6831±2.3178 (1.00) |
+1μM Dacomitinb | 4.8224±0.9831 (0.75) | 9.1475±1.8112 (1.05) |
S1 | S1-MI-80 (ABCG2) | |
MX | 0.1715±0.0262 (1.00) | 8.5372±0.7831 (1.00) |
+0.25μM Dacomitinb | 0.1571±0.0144 (1.09) | 1.6636±0.2819 (5.13)** |
+0.5μM Dacomitinb | 0.1369±0.0042 (1.25) | 1.1503±0.0709 (7.42)** |
+1μM Dacomitinb | 0.1529±0.0018 (1.12) | 0.6009±0.0128 (14.20)** |
+2.5μM FTC | 0.1405±0.0494 (1.22) | 2.2289±0.3450 (3.83)** |
Topotecan | 0.7334±0.0785 (1.00) | 83.1904±2.4666 (1.00) |
+0.25μM Dacomitinb | 0.9914±0.3053 (0.74) | 72.2940±8.0594 (1.15) |
+0.5μM Dacomitinb | 0.5367±0.0921 (1.36) | 15.9879±1.9511 (5.18)** |
+1μM Dacomitinb | 0.7060±0.0407 (1.03) | 11.4639±1.0595 (7.24)** |
+2.5μM FTC | 0.8681±0.0611 (0.85) | 7.7162±0.5868 (10.75)** |
DDP | 11.1384±1.6603 (1.00) | 11.0324±0.1046 (1.00) |
+1μM Dacomitinb | 10.8398±1.0169 (1.02) | 12.1685±0.7354 (0.90) |