product name Trifluridine
Description: Trifluridine (also known as trifluorothymidine or TFT, NSC 529182, NSC 75520) is an anti-herpesvirus antiviral agent 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. It is a component of the experimental anti-cancer drug TAS-102.
References: Cancer Chemother Pharmacol. 2015 Aug;76(2):325-33; Invest Ophthalmol Vis Sci. 1989 Apr;30(4):678-83.
296.2
Formula
C10H11F3N2O5
CAS No.
70-00-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 59 mg/mL (199.2 mM)
Water: 59 mg/mL (199.2 mM)
Ethanol: 59 mg/mL (199.2 mM)
Solubility (In vivo)
Synonyms
NSC 529182, NSC 75520
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413143
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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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| Formulation & Dosage | |
| References | Cancer Chemother Pharmacol. 2015 Aug;76(2):325-33; Invest Ophthalmol Vis Sci. 1989 Apr;30(4):678-83. |
