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抑制剂描述：

产品名称：Trifluorothymidine

产品别名：见爱必信官网

英文别名：Trifluorothymidine

靶点：Thymidylate Synthase

CAS：70-00-8

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：

Trifluridine (Viroptic) is an anti-herpesvirus antiviral drug, used primarily on the eye. It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the -CF3 group added to the uracil component blocks base pairing.

溶解性：DMSO ：29.6 mg/mL (100 mM)
Water ：14.8 mg/mL (50 mM)

体外研究：

Trifluridine inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. Trifluridine inhibits colony formation of bone marrow cells in a concentration-dependent manner. Trifluridine (FTD) and 2'-deoxy-5-fluorouridine (FdUrd) are incorporated into DNA with different efficiencies due to differences in the substrate specificities of TK1 and DUT, causing abundant FTD incorporation into DNA. FTD-treated cells shows differing nuclear morphologies compared to FdUrd-treated cells. Trifluridine inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently.

体内研究：Trifluridine has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits. Trifluridine has increased antitumor activity and is incorporated into DNA more effectively than continuously infused Trifluridine in mice. Trifluridine gradually accumulates in tumor cell DNA, in a TPI-independent manner, and significantly delays tumor growth and prolonged survival in mice, compared to treatment with 5-FU derivatives. Trifluridine results in significantly lower viral titers, fewer HSV-1-positive eyes/total during the treatment period, lower keratitis scores, fewer eyes with keratitis/total, and a shorter time to resolution of keratitis in the New Zealand rabbit ocular model.

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