Trifluorothymidine

DNA synthesis

296.2

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

白色至淡黄色粉末

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.

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.

曲氟胸苷;Trifluridine; FTD; 5-Trifluorothymidine; NSC 529182; NSC 75520

C₁₀H₁₁F₃N₂O₅

70-00-8