Trifluridine (NSC 75520)

Synonyms: NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT

Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.

Trifluridine (NSC 75520) Chemical Structure

Trifluridine (NSC 75520) Chemical Structure

CAS: 70-00-8

Selleck's Trifluridine (NSC 75520) has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

Choose Selective Thymidylate Synthase Inhibitors

Biological Activity

Description Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.
Targets
DNA synthesis [1]
In vitro
In vitro 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. [1] 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. [2] Trifluridine inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. [3]
In Vivo
In vivo Trifluridine has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits. [4] 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. [5] 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. [6]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06039202 Not yet recruiting Metastatic Colorectal Cancer Holy Stone Healthcare Co. Ltd January 2024 Phase 2
NCT05228184 Recruiting Congenital Hypothyroidism IBSA Institut Biochimique SA|Cromsource January 21 2022 Phase 4
NCT04944017 Recruiting Parkinson''s Disease|Depression Yale University|Fox (Michael J.) Foundation for Parkinson''s Research November 23 2021 Phase 2
NCT04554836 Active not recruiting Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum TheraOp December 29 2020 Phase 2
NCT04166604 Recruiting Metastatic Colorectal Cancer GERCOR - Multidisciplinary Oncology Cooperative Group May 20 2020 Phase 2

Chemical lnformation & Solubility

Molecular Weight 296.2 Formula

C10H11F3N2O5

CAS No. 70-00-8 SDF Download Trifluridine (NSC 75520) SDF
Smiles C1C(C(OC1N2C=C(C(=O)NC2=O)C(F)(F)F)CO)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (199.18 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 59 mg/mL

Ethanol : 59 mg/mL


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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