Table 1.
Treatment | HEK293/pcDNA3.1 | ABCG2-482-R2 | |||||||
---|---|---|---|---|---|---|---|---|---|
IC50(nM) | FR a | IC50(nM) | FR a | ||||||
Mitoxantrone | 17.77 | ± | 1.34 | 1.00 | 227.40 | ± | 14.95 | 12.80 | |
+OSI-930 | 10 µM | 23.17 | ± | 3.37 | 1.30 | 42.24 | ± | 17.56 | 2.38 |
+VKJP1 | 10 µM | 11.28 | ± | 1.23 | 0.63 | 14.90 | ± | 8.70 | 0.84 |
+VKJP2 | 10 µM | 18.95 | ± | 7.45 | 1.07 | 61.81 | ± | 14.77 | 3.48 |
+VKJP3 | 10 µM | 10.68 | ± | 0.84 | 0.60 | 35.15 | ± | 11.96 | 1.98 |
+VKJP4 | 10 µM | 17.24 | ± | 2.96 | 0.97 | 58.95 | ± | 0.94 | 3.32 |
+VKJP5 | 10 µM | 14.93 | ± | 0.92 | 0.84 | 50.59 | ± | 5.57 | 2.85 |
+VKJP6 | 10 µM | 20.42 | ± | 0.69 | 1.15 | 61.88 | ± | 9.23 | 3.48 |
+VKJP7 | 10 µM | 15.64 | ± | 4.01 | 0.88 | 67.21 | ± | 11.78 | 3.78 |
+VKJP8 | 10 µM | 16.40 | ± | 3.35 | 0.92 | 79.48 | ± | 20.81 | 4.47 |
+VKJP9 | 10 µM | 18.32 | ± | 8.31 | 1.03 | 54.82 | ± | 24.55 | 3.08 |
+VKJP10 | 10 µM | 17.35 | ± | 8.45 | 0.98 | 53.93 | ± | 25.04 | 3.03 |
+VKJP11 | 10 µM | 15.72 | ± | 1.94 | 0.88 | 65.34 | ± | 25.35 | 3.68 |
+VKJP12 | 10 µM | 22.36 | ± | 6.90 | 1.26 | 54.66 | ± | 17.06 | 3.08 |
+VKJP13 | 10 µM | 17.96 | ± | 1.40 | 1.01 | 217.52 | ± | 18.65 | 12.20 |
+VKJP14 | 10 µM | 19.97 | ± | 5.74 | 1.12 | 257.63 | ± | 35.88 | 14.50 |
+VKJP15 | 10 µM | 14.51 | ± | 2.49 | 0.82 | 57.05 | ± | 26.69 | 3.21 |
+FTC | 2.5 µM | 16.15 | ± | 1.19 | 0.91 | 20.17 | ± | 2.38 | 1.14 |
Fold-resistance was determined by dividing the IC50 value for mitoxantrone of ABCG2-482-R2 cells by IC50 value of HEK293/pcDNA3.1 cells in the absence or presence of the test compounds or FTC.