Table 1. Cytotoxic activity of KP772 against various cell models at 72 h treatment.
| Cell line | Overexpressed protein | Fold resistancea | IC75 (μM) |
IC50 (μM) |
IC25 (μM) |
|||
|---|---|---|---|---|---|---|---|---|
| Meanb | ±S.D. | Meanb | ±S.D. | Meanb | ±S.D. | |||
| GLC-4 | Parental | - | 0.92 | 0.03 | 1.31 | 0.03 | 2.16 | 0.04 |
| GLC-4/adr | ABCC1, LRP | 0.61*** | 0.64 | 0.03 | 0.80 | 0.02 | 0.96 | 0.02 |
| HL60 | Parental | - | 1.33 | 0.58 | 1.77 | 0.04 | 2.20 | 0.03 |
| HL60/adr | ABCC1 | 0.44*** | 0.46 | 0.09 | 0.78 | 0.04 | 2.26 | 0.31 |
| KB-3-1 | Parental | - | 1.68 | 0.06 | 2.49 | 0.24 | 4.93 | 0.06 |
| KBC-1 | ABCB1 | 0.50* | 0.82 | 0.03 | 1.43 | 0.17 | 3.51 | 0.44 |
| MCF-7 | Parental | - | 1.6 | 0.24 | 4.29 | 0.43 | >10.0 | - |
| MCF-7/bcrp | ABCG2 | 0.54* | 0.31 | 0.03 | 2.33* | 0.21 | >10.0 | - |
| A459 | ABCC1, ABCC2, ABCG2, LRP | - | 0.9 | 0.1 | 1.5 | 0.10 | 2.6 | 0.2 |
a
Differences in KP772 sensitivity calculated by dividing IC50 values of the MDR subline by those of the parental cell lines.
b
IC75, IC50, and IC25 were calculated from whole dose–response curves. Values given are means ± S.D. of 1 representative experiment out of three, performed in triplicates.
*
Significantly different from parental cell line ( p < 0.05).
***
Significantly different from parental cell line ( p < 0.001).