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The biological activity of TOP2A inhibitors using SW620 tumor organoid models of TCF-transcription, 3D cell viability, and EMT reporters of vimentin and E-cadherin.
| Analog | TCF Inhibition IC50 (μM) | Cytotoxicity (CellTox Green) EC50 (μM) | Vimentin downregulation EC50 (μM) | E-cadherin upregulation EC50 (μM) |
|---|---|---|---|---|
| 3 | 2.4 | >30 | 4 | 9 |
| 7 | 2.4 | >30 | 1.2 | 1.6 |
| 35 | 2.0 | >30 | 9.5 | 5.5 |
| 39 | 4.7 | >30 | 4.7 | 3.1 |
| 42 | 0.7 | 16 | 1.9 | 1.2 |
| 53 | 1.0 | > 30 | 3.5 | 5.4 |
| 56 | 1.7 | >30 | 1.7 | 3.4 |
| 57 | 5.0 | >30 | 1.2 | 1.1 |
| 60 | 1.1 | 22 | 1.0 | 3.3 |
| 61 | 2.5 | 17.4 | 2.4 | 3.0 |
