| Bioactivity | RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells[1]. |
| Formula | C20H16F7N3O3 |
| Molar Mass | 479.35 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fried W, et al. Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors. Nat Commun. 2024 Apr 5;15(1):2862. |