产品
编 号:F430414
分子式:C10H11F3N2O5
分子量:296.2
产品类型
结构图
CAS No: 70-00-8
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产品详情
生物活性:
Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.
体内研究:
Trifluridine/tipiracil (200 mg/kg,口服,每天两次,连续 5 天,然后 2 天不用药,持续 6 周) 在人结直肠腹膜内异种移植模型中显示出抗肿瘤活性。Trifluridine (75 或 150 mg/kg,口服灌胃,每天一次,连续 5 天) 抑制植入的小鼠 TNBC 肿瘤的生长。Animal Model:Nude mice (human colorectal intraperitoneal xenograft model)
Dosage: 200 mg/kg(trifluridine/tipiracil)
Administration:Oral administration; Once a day; 5 days followed by 2 drug-free days, a total of 6 weeks
Result:Exhibited a significantly longer survival time compared with untreated mice.
Animal Model:Mouse model of breast cancer
Dosage:75 or 150 mg/kg
Administration:Oral gavage; daily for 10 days
Result:Treatment with different doses inhibited the growth of TNBC tumors in mouse in a dose-dependent manner
Animal Model:The human gastric MKN45 intraperitoneal xenograft model
Dosage:200 mg/kg (Trifluridine/tipiracil)
Administration:twice daily for 5 consecutive days followed by 2 drug?free days for 6 weeks
Result:Prolonged the survival of mice compared with untreated mice.
体外研究:
Trifluridine (0.5 μM,3 天) 诱导 HUVEC 细胞衰老。Trifluridine (0.5 μM,3 天) 通过 mTOR 途径抑制 HUVEC 中的自噬和自噬通量。Trifluridine (0-5 μM,3 天) 以浓度依赖性方式抑制 HUVEC 细胞活力。Trifluridine (5 μM-20 μM,24 h–72 h) 抑制 MCF-7、MDA-MB-231、BT-549 和 Hs578T 的增殖。Trifluridine (0 μM-20 μM,48 小时) 选择性诱导 MCF-7、MDA-MB-231、BT-549 和 Hs578T 细胞凋亡。Trifluridine (10 μM,72 小时) 可诱导 MCF-10A、MCF-7、MDA-MB-231 和 BT-549 细胞中的 DNA 双链断裂。