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Fig. 4 | Journal of Experimental & Clinical Cancer Research

Fig. 4

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

Fig. 4

Effect of dacomitinib on the efflux of Rho 123, the ATPase activity and the[125I]-IAAP photoaffinity labeling of ABCG2. Time course of Rho 123 efflux was measured in S1 and S1-80-MI cells, with or without 1 μM dacomitinib (a). dacomitinib competed for photolabeling of ABCG2 by [125I]-IAAP (b). Crude membranes from MCF7/FLV1000 cells overexpressing ABCG2 were incubated with [125I]-IAAP and a range of different concentration (0–10 μM) of dacomitinib. The samples were then cross-linked by UV illumination, subjected to SDS-PAGE, and analyzed as described in Materials and Methods. A representative autoradiogram from three independent experiments was shown. The relative amount of [125I]-IAAP incorporated was plotted against the concentration of dacomitinib used in the competition. 100% incorporation refered to the absence of dacomitinib. Effect of dacomitinib on ABCG2 ATPase activity (c). The vanadate-sensitive ABCG2 ATPase activity in the presence of the indicated concentrations of dacomitinib was evaluated. The mean and standard error values from three independent experiments were shown

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