2. Apoptosis Anti-infection Cell Cycle/DNA Damage Autophagy
  3. Thymidylate Synthase HSV Nucleoside Antimetabolite/Analog Orthopoxvirus DNA/RNA Synthesis Apoptosis Autophagy
  4. Trifluridine

Trifluridine  (Synonyms: Trifluorothymidine; 5-Trifluorothymidine; TFT)

Cat. No.: HY-A0061 Purity: 99.83%
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Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.

For research use only. We do not sell to patients.

Trifluridine Chemical Structure

Trifluridine Chemical Structure

CAS No. : 70-00-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
50 mg USD 84 In-stock
100 mg USD 126 In-stock
200 mg USD 192 In-stock
500 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

Other Forms of Trifluridine:

Trifluridine Related Antibodies

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1 Publications Citing Use of MCE Trifluridine

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors[1][2][3][4].

IC50 & Target[1][2][3][4]

Thymidylate Synthase

 

Nucleoside Antimetabolite/Analog

 

HSV-1

 

HSV-2

 

In Vitro

Trifluridine (0.5 μΜ, 3 days) induces cellular senescence in HUVECs[2].
Trifluridine (0.5 μΜ, 3 days) inhibits autophagy and autophagy flux via the mTOR pathway in HUVECs [2].
Trifluridine (0-5 μΜ, 3 days) inhibits HUVEC cells viability in a concentration-dependent way[2].
Trifluridine (5 µM-20 µM, 24 h–72 h) inhibits the proliferation in MCF-7, MDA-MB-231, BT-549 and Hs578T[4].
Trifluridine (0 µM-20 µM, 48 h) selectively induces apoptosis in MCF-7, MDA-MB-231, BT-549 and Hs578T cells [4].
Trifluridine (10 µM, 72 h) induces DNA double-strand break in MCF-10A, MCF-7, MDA-MB-231 and BT-549 cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trifluridine Related Antibodies

Cell Viability Assay[2]

Cell Line: HUVEC cells
Concentration: 0-5 μM
Incubation Time: 3 days
Result: Cell viability dropped sharply at 3 μM and 5 μM.

Immunofluorescence[2]

Cell Line: HUVEC cells
Concentration: 0-5 μM
Incubation Time: 3 days
Result: Induced cellular senescence by inhibiting autophagy flux.

Western Blot Analysis[2]

Cell Line: HUVEC cells
Concentration: 0-5 μM
Incubation Time: 3 days
Result: Increased protein levels of senescence markers: p53, p16, SASP (IL-1, IL-6, TNF-α, p21).

Cell Proliferation Assay[4]

Cell Line: MCF-7, MDA-MB-231, BT-549, Hs578T and MCF-10A(control non-tumor) cells
Concentration: 5 µM-20 µM
Incubation Time: 24 h–72 h
Result: Inhibited the proliferation of MDA-MB231, BT549 and Hs578T cells at 10µM and 20µM, significantly.

Apoptosis Analysis[4]

Cell Line: MDA-MB-231, BT-549, and Hs578T cells
Concentration: 10µM or 20 µM
Incubation Time: 48 h
Result: Increased the percentages of apoptotic TNBC cells (MDA-MB-231, BT-549, and Hs578Tcells) at 10µM and 20µM, significantly.
In Vivo

Trifluridine/tipiracil (200 mg/kg, PO, twice daily for 5 consecutive days followed by 2 drug-free days for 6 weeks) shows antitumor activity in the human colorectal intraperitoneal xenograft model[3].
Trifluridine (75 or 150 mg/kg, oral gavage, once daily for 5 consecutive days) inhibits the growth in implanted mouse TNBC tumors [4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (human colorectal intraperitoneal xenograft model)[3]
Dosage: 200 mg/kg(trifluridine/tipiracil)
Administration: Oral administration; Once a day; 5 days followed by 2 drug-free days, a total of 6 weeks
Result: Exhibited a significantly longer survival time compared with untreated mice.
Animal Model: Mouse model of breast cancer[4]
Dosage: 75 or 150 mg/kg
Administration: Oral gavage; daily for 10 days
Result: Treatment with different doses inhibited the growth of TNBC tumors in mouse in a dose-dependent manner
Animal Model: The human gastric MKN45 intraperitoneal xenograft model[3]
Dosage: 200 mg/kg (Trifluridine/tipiracil)
Administration: twice daily for 5 consecutive days followed by 2 drug‑free days for 6 weeks
Result: Prolonged the survival of mice compared with untreated mice.
Clinical Trial
Molecular Weight

296.20

Formula

C10H11F3N2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1C[C@H](N2C(NC(C(C(F)(F)F)=C2)=O)=O)O[C@@H]1CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (337.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (112.53 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3761 mL 16.8805 mL 33.7610 mL
5 mM 0.6752 mL 3.3761 mL 6.7522 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.98%

COA (254 KB) HNMR (154 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.3761 mL 16.8805 mL 33.7610 mL 84.4024 mL
5 mM 0.6752 mL 3.3761 mL 6.7522 mL 16.8805 mL
10 mM 0.3376 mL 1.6880 mL 3.3761 mL 8.4402 mL
15 mM 0.2251 mL 1.1254 mL 2.2507 mL 5.6268 mL
20 mM 0.1688 mL 0.8440 mL 1.6880 mL 4.2201 mL
25 mM 0.1350 mL 0.6752 mL 1.3504 mL 3.3761 mL
30 mM 0.1125 mL 0.5627 mL 1.1254 mL 2.8134 mL
40 mM 0.0844 mL 0.4220 mL 0.8440 mL 2.1101 mL
50 mM 0.0675 mL 0.3376 mL 0.6752 mL 1.6880 mL
60 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
80 mM 0.0422 mL 0.2110 mL 0.4220 mL 1.0550 mL
100 mM 0.0338 mL 0.1688 mL 0.3376 mL 0.8440 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Trifluridine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trifluridine70-00-8Trifluorothymidine 5-Trifluorothymidine TFTThymidylate SynthaseHSVNucleoside Antimetabolite/AnalogOrthopoxvirusDNA/RNA SynthesisApoptosisAutophagyHerpes simplex virusmTORantitumorantiviralHUVECcancermetastatic colorectal cancergastrointestinal tumorInhibitorinhibitorinhibit

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