Table 1.
Cytotoxic selectivity of AA3266 and reference compounds. Average (±S.D.) readout reductions (compared to control) in cell counting and MTT assays, after incubation with 100 µM.
| Cmpd | Description | Cell Counting | MTT | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Readout Reduction (at 100 µM) [Percentage Points] 1 | Selectivity 2 | Readout Reduction (at 100 µM) [Percentage Points] 1 | Selectivity 2 | ||||||
| Melanoma 3 | All Cancers 4 | Normal Cells 5 | Melanoma 3 | All Cancers 4 | Normal Cells 5 | ||||
| AA3266 This paper and [29] |
potent µOR and δOR agonist; moderate NK1 antagonist | 61 ± 16 | 44 ± 25 | 18 ± 5 | 3.4 / 2.5 | 42 ± 9 | 44 ± 15 | 17 ± 13 | 2.5 / 2.6 |
| AWL3020 [44] |
potent δOR agonist; low µOR and NK1R binding | 51 ± 26 | 47 ± 19 | 33 ± 6 | 1.6 / 1.4 | 38 ± 21 | 44 ± 20 | 43 ± 6 | 0.9 / 1.0 |
| Aprepitant [29,45] |
potent NK1-antagonist | 36 ± 3 | 37 ± 2 | 32 ± 4 | 1.1 / 1.2 | 40 ± 16 | 38 ± 12 | 28 ± 5 | 1.4 / 1.3 |
1 Readout reduction expressed in percentage points, obtained by subtracting the normalized readout for a particular compound from the control value (100%), 2 selectivity is calculated by dividing the reduction observed in either the melanoma group or all cancers group by the reduction observed in normal cells group, 3 MeW164, MeW155 and MeW151 cell lines, 4 MeW164, MeW155, MeW151, E14, T24 cell lines, 5 Fib9, FlW180 and FlWp95 cell lines.