Name: Polθ/PARP-IN-1
Brand: TargetMol
SKU: T209387
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

生物活性

产品描述	Polθ/PARP-IN-1 (compound 25d) is a potent dual inhibitor of DNA polymerase theta (Polθ) and PARP, with IC50 values of 45.6 nM and 5.4 nM, respectively. This compound exhibits antiproliferative activity, induces apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage, and demonstrates antitumor properties.
体外活性	Polθ/PARP-IN-1 (compound 25d) (0-80 µM; 3天) 对HCC1937、MDA-MB-436、HCT116、SW48、SKOV-3、MCF-10A 显示良好的抗增殖活性，IC 50值分别为20.9、2.7、8.9、2.9、18.9、>80 µM。此外， Polθ/PARP-IN-1 (compound 25d) (2 µM; 3天) 可诱导细胞凋亡及在G2/M期的细胞周期停滞，从而导致DNA损伤。
体内活性	Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; 连续21天每日给药) 能抑制 MDA-MB-436 异种移植模型的肿瘤生长。