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. 2012 Jul;82(1):47–58. doi: 10.1124/mol.111.076299

TABLE 2.

Effects of neratinib in reversing ABCB1-mediated MDR in transfected cell lines

Cell survival rates were determined with MTT assays, as described under Materials and Methods. Data are the mean ± S.D. of at least three independent experiments performed in triplicate. The fold reversal of MDR was calculated by dividing the IC50 for cells with the anticancer drug in the absence of inhibitor by that in the presence of inhibitor.

Compounds IC50 (Reversal)
HEK293/pcDNA3.1 HEK293/ABCB1
μM (fold)
Doxorubicin 0.074 ± 0.006 (1.00) 1.339 ± 0.130 (1.00)
    + 0.25 μM Neratinib 0.065 ± 0.006 (1.13) 0.756 ± 0.070 (1.77)**
    + 0.5 μM Neratinib 0.079 ± 0.008 (0.94) 0.332 ± 0.027 (4.03)**
    + 1.0 μM Neratinib 0.082 ± 0.007 (0.90) 0.167 ± 0.010 (7.98)**
    + 10 μM Verapamil 0.083 ± 0.008 (0.89) 0.094 ± 0.008 (14.19)**
Cisplatin 2.431 ± 0.27 (1.00) 2.681 ± 0.27 (1.00)
    + 1.0 μM Neratinib 2.263 ± 0.22 (1.07) 2.176 ± 0.22 (1.23)
    + 10 μM Verapamil 2.356 ± 0.23 (1.03) 2.344 ± 0.23 (1.14)
**

P < 0.01 versus the values obtained in the absence of inhibitor.