Table 1. The effect of various compounds on the proliferation of A2780wt and A2780.140 cells in the presence and absence of novobiocin, a BCRP inhibitor.
|
IC50 (nM)
|
||||
|---|---|---|---|---|
| Compound | A2780wt | A2780.140 | R.F. (no BCRP inhibitor) | R.F. (+60 μM novobiocin) |
| STX66 | 500 | 590 | 1.2 | nd |
| STX68 | 410 | 380 | 0.9 | nd |
| STX138 | 400 | 400 | 1.0 | nd |
| STX140 | 240 | 1930 | 7.9 | 1.5 |
| STX243 | 260 | 830 | 3.2 | nd |
| STX260 | 230 | 1170 | 5.0 | 1.9 |
| STX640 | 320 | 320 | 1.0 | nd |
| STX641 | 40 | 50 | 1.2 | 1.2 |
| STX564 | 180 | 170 | 0.9 | nd |
| Taxol | 6 | 4 | 0.7 | nd |
| Colchicine | 4 | 5 | 1.1 | nd |
| MXR | 150 | 940 | 6.5 | 2.4 |
| DOX | 170 | 570 | 3.3 | 1.2 |
Cells were treated in triplicate with a range of concentrations of the compounds in the presence or absence of 60 μM novobiocin. After 4 days proliferation was measured using the CellTiter96 Aqueous One assay (Promega) and the IC50 values were calculated. Results are representative of at least two separate experiments (IC50=nM; R.F.=resistance factor (=IC50 A2780.140/IC50 A2780wt); nd=not determined).