Description

Product Description

Trifluridine, also known as 5-trifluoromethyl-2′-deoxyuridine, is a thymidine analog in which the methyl group on the pyrimidine ring is substituted by a trifluoromethyl group. This modification gives Trifluridine potent biochemical activity as an inhibitor of DNA synthesis.

In research, Trifluridine is primarily used to:

• Study the mechanisms of DNA polymerase inhibition.

• Explore nucleoside analog incorporation into viral or cancer cell DNA.

• Investigate fluoropyrimidine-induced cytotoxicity and replication stress in proliferating cells.

• Model antiviral and anticancer nucleoside metabolism.

Mechanistically, Trifluridine undergoes phosphorylation to its active triphosphate form (TF-TTP) by thymidine kinase (TK). The triphosphate derivative competes with thymidine triphosphate for incorporation into DNA, leading to base mispairing, DNA strand breaks, and inhibition of DNA synthesis. In viral research, Trifluridine demonstrates inhibitory activity against DNA viruses, such as herpes simplex virus (HSV), by interfering with viral DNA polymerase function.

In oncology research, Trifluridine is a key component of the combination drug trifluridine/tipiracil, designed to improve stability and bioavailability in preclinical and clinical models. This pairing enables sustained exposure to the active metabolite, facilitating studies of nucleoside analog synergy, DNA repair response, and tumor proliferation control.

Product Specifications

Mechanism of Action

Trifluridine’s biological activity is derived from its mimicry of thymidine, allowing incorporation into DNA during replication.

1. Phosphorylation and Activation

Trifluridine is converted intracellularly by thymidine kinase to its monophosphate, diphosphate, and triphosphate derivatives. The active form, TF-TTP, competes with thymidine triphosphate for DNA polymerase-mediated incorporation.

2. DNA Incorporation and Misincorporation

Once incorporated, the trifluoromethyl group alters base pairing and hydrogen bonding, disrupting DNA replication fidelity. This process triggers replication fork collapse and DNA damage signaling pathways.

3. Inhibition of DNA Synthesis

Through competitive inhibition, Trifluridine reduces DNA chain elongation and overall DNA synthesis rates, particularly in rapidly dividing or virally infected cells.

4. Viral DNA Polymerase Interference

Trifluridine inhibits viral DNA polymerase more effectively than host enzymes, leading to suppression of viral replication — especially in herpes simplex virus (HSV) studies.

5. Research Applications

• Mechanistic studies of fluorinated nucleosides.

• Analysis of DNA polymerase kinetics and fidelity.

• Examination of DNA repair pathways and replication stress markers.

• Evaluation of antiviral and cytotoxic synergy with other nucleoside analogs or polymerase inhibitors.

  

Side Effects

In preclinical or in vitro studies, Trifluridine exposure can lead to:

• DNA strand breaks and replication arrest.

• Cytotoxicity in rapidly dividing cells.

• Altered mitochondrial DNA synthesis at high concentrations.

• Oxidative stress and p53 pathway activation.

These effects are valuable for mechanistic exploration but emphasize that Trifluridine is for laboratory research use only, not for therapeutic or diagnostic purposes.

Keywords

Trifluridine, CAS 70-00-8, fluorinated thymidine analog, nucleoside analog research, antiviral compound, anticancer nucleoside, DNA synthesis inhibitor, fluoropyrimidine study, viral polymerase inhibitor, DNA incorporation research, high-purity nucleoside analog, OEM & bulk nucleoside supplier China.

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Disclaimer

All products listed are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostics and should not be administered to humans or animals. Researchers must handle all materials in accordance with institutional biosafety and chemical safety guidelines. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval.