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Table 2 Effect of dacomitinib on reversing and ABCG2-mediated MDR in stable-transfected cells

From: Dacomitinib potentiates the efficacy of conventional chemotherapeutic agents via inhibiting the drug efflux function of ABCG2 in vitro and in vivo

Compounds

IC50±SD (μM) (fold-reversal)

HEK293/pcDNA3.1

ABCG2-482-R2

ABCG2-482-T7

MX

0.0093±0.0012 (1.00)

0.0762±0.0020 (1.00)

0.0356±0.0266 (1.00)

+0.25μM Dacomitinib

0.0072±0.0004 (1.29)

0.0340±0.0026 (2.22)**

0.0171±0.0005 (2.08)**

+0.5μM Dacomitinib

0.0097±0.0003 (0.95)

0.0230±0.0011 (3.27)**

0.0098±0.0009 (3.63)**

+1μM Dacomitinib

0.0074±0.0001 (1.25)

0.0150±0.0021 (5.08)**

0.0092±0.0008 (3.86)**

+2.5μM FTC

0.0106±0.0016 (0.87)

0.0060±0.0013 (12.09)**

0.0025±0.0029 (12.40)**

DDP

2.5420±0.1392 (1.00)

1.0719±0.1109 (1.00)

0.8525±0.0502 (1.00)

+1μM Dacomitinb

2.2230±0.0433 (1.14)

0.9194±0.0177 (1.16)

0.9150±0.1908 (0.93)

  1. Cell survival was performed by MTT assay as described in “Materials and Methods”. VRP (specific inhibitor of ABCB1) and FTC (specific inhibitor of ABCG2) were used as the positive control. The fold reversal of MDR (values given in parentheses) was calculated by dividing the IC50 value for cells with the anticancer agent in the absence of dacomitinib by that obtained in the presence of dacomitinib. Data were shown as the mean ± SD of at least three independent experiments performed in triplicate. *p < 0.05, **p < 0.01
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Journal of Experimental & Clinical Cancer Research

ISSN: 1756-9966

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