Trifluridine

Catalog No.S1778 Synonyms: NSC 529182, NSC 75520

Trifluridine  Chemical Structure

Molecular Weight(MW): 296.2

Trifluridine is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Trifluridine is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.
Targets
DNA synthesis [1]
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 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]

Protocol

Solubility (25°C)

In vitro DMSO 59 mg/mL (199.18 mM)
Water 59 mg/mL warmed (199.18 mM)
Ethanol 59 mg/mL (199.18 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 296.2
Formula

C10H11F3N2O5

CAS No. 70-00-8
Storage powder
Synonyms NSC 529182, NSC 75520

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03031691 Not yet recruiting Metastatic Colorectal Cancer OncoMed Pharmaceuticals, Inc. January 2017 Phase 1
NCT02848443 Recruiting Metastatic Colorectal Cancer Institut de Recherches Internationales Servier|Servier May 2016 Phase 1
NCT02743221 Recruiting Metastatic Colorectal Cancer Institut de Recherches Internationales Servier|Servier April 2016 Phase 2
NCT01867866 Active, not recruiting Advanced Solid Tumors Taiho Oncology, Inc. June 2013 Phase 1
NCT00000635 Completed Herpes Simplex|HIV Infections National Institute of Allergy and Infectious Diseases (NIAID)|Glaxo Wellcome null --
NCT00002037 Completed Mycobacterium Avium-Intracellulare Infection|HIV Infections Amgen|NIH AIDS Clinical Trials Information Service null --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID