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. 2016 Sep 15;21(9):1236. doi: 10.3390/molecules21091236

Table 1.

Reversal effects of osimertinib on ABCB1-mediated MDR in KB-3-1 and KB-C2 cell lines.

Treatment KB-3-1 KB-C2
IC50 ± SD a (nM) RF b IC50 ± SD (µM) RF
Paclitaxel 3.58 ± 0.35 [1.0] 1.075 ± 0.299 [307.1]
+ Osimertinib (0.3 µM) 3.63 ± 0.49 [1.0] 0.603 ± 0.045 * [172.3]
+ Osimertinib (0.5 µM) 3.57 ± 0.41 [1.0] 0.092 ± 0.008 * [26.3]
+ Osimertinib (1.0 µM) 3.12 ± 0.47 [0.9] 0.017 ± 0.005 * [4.9]
+ Verapamil (3.0 µM) 3.24 ± 0.44 [0.9] 0.056 ± 0.011 * [16.0]
+ Zosuquidar (0.3 µM) 2.81 ± 0.36 [0.8] 0.013 ± 0.003 * [3.7]
Colchicine 59.82 ± 8.57 [1.0] 15.528 ± 4.565 [259.6]
+ Osimertinib (0.3 µM) 56.60 ± 7.13 [0.9] 5.120 ± 0.982 * [85.6]
+ Osimertinib (0.5 µM) 58.66 ± 5.20 [1.0] 1.279 ± 0.606 * [21.4]
+ Osimertinib (1.0 µM) 52.53 ± 7.39 [0.9] 0.637 ± 0.071 * [10.6]
+ Verapamil (3.0 µM) 58.87 ± 9.65 [1.0] 0.279 ± 0.015 * [4.7]
+ Zosuquidar (0.3 µM) 52.54 ± 9.12 [0.9] 0.078 ± 0.020 * [3.7]
Vincristine 5.05 ± 0.89 [1.0] 0.797 ± 0.019 [157.8]
+ Osimertinib (0.3 µM) 5.49 ± 0.54 [1.1] 0.789 ± 0.027 [156.3]
+ Osimertinib (0.5 µM) 5.26 ± 0.71 [1.0] 0.228 ± 0.037 * [45.1]
+ Osimertinib (1.0 µM) 5.56 ± 0.96 [1.1] 0.027 ± 0.006 * [5.2]
+ Verapamil (3.0 µM) 4.61 ± 0.86 [0.9] 0.062 ± 0.008 * [12.3]
+ Zosuquidar (0.3 µM) 4.58 ± 0.65 [0.9] 0.013 ± 0.003 * [2.6]
IC50 ± SD (µM) RF IC50 ± SD (µM) RF
Cisplatin 2.90 ± 0.27 [1.0] 3.12 ± 0.20 [1.1]
+ Osimertinib (1.0 µM) 2.78 ± 0.17 [1.0] 2.98 ± 0.22 [1.0]
+ Verapamil (3.0 µM) 2.61 ± 0.20 [0.9] 2.66 ± 0.31 [0.9]

a IC50 values are represented as mean ± SD of at least three independent experiments performed in triplicate; b Values represent the resistance fold (RF) obtained by dividing IC50 value of anticancer drug in KB-3-1 and KB-C2 cells with or without reversal agent divided by the IC50 value of the respective anticancer drug in KB-3-1 cells without reversal agent. * p < 0.01 versus the control group.