| Bioactivity | Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity[1]. |
| Invitro | Polθ/PARP-IN-1 (compound 25d) (0-80 µM; 3 days) 对 HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A 显示出抗增殖活性，IC50 值分别为 20.9、2.7、8.9、2.9、18.9、>80 µM[1]。Polθ/PARP-IN-1 (compound 25d) (2 µM; 3 days) 诱导细胞凋亡和细胞周期停滞在 G2/M 期，导致 DNA 损伤[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Polθ/PARP-IN-1 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; daily for 21 consecutive days) 可抑制 MDA-MB-436 异种移植模型中的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C38H33ClFN7O5S |
| Molar Mass | 754.23 |
| 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]. Ma L, et al. Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors. J Med Chem. 2024 Feb 20. |