Art. -Nr.: HY-A0061

Trifluridine

(Synonyms: Trifluorothymidine; 5-Trifluorothymidine; TFT)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 99.96%
CAS. Nr.: 70-00-8
Formel: C₁₀H₁₁F₃N₂O₅
Molecular Weight:296.20

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Trifluridine Chemical Structure

CAS. Nr.: 70-00-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[3]^[4]

Thymidylate Synthase

Nucleoside Antimetabolite/Analog

HSV-1

HSV-2

Alle HSV Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	EC₅₀	3.37 μM Compound: 25	Antiviral activity against DHBV infected in duck hepatocytes assessed as inhibition of viral DNA replication Antiviral activity against DHBV infected in duck hepatocytes assessed as inhibition of viral DNA replication	[PMID: 20857959]
HepG2 2.2.15	EC₅₀	10 μg/mL Compound: 2	Antiviral activity against HBV infected in human 2.2.15 cell at 10 ug/ml Antiviral activity against HBV infected in human 2.2.15 cell at 10 ug/ml	[PMID: 20863701]
Huh-7	CC₅₀	>675 μM Compound: 25	Cytotoxicity against HuH7 cells Cytotoxicity against HuH7 cells	[PMID: 20857959]
Huh-7	CC₅₀	>200 μg/mL Compound: 2	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 20863701]
Vero	CC₅₀	50.6 μM Compound: TFT	Cytotoxicity against african green monkey Vero cells after 2 days Cytotoxicity against african green monkey Vero cells after 2 days	[PMID: 17438061]
Vero	EC₅₀	<1.7 μM Compound: TFT	Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs	[PMID: 17438061]
Vero	EC₅₀	1.7 μM Compound: TFT	Antiviral activity against Herpes B virus 24105 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs Antiviral activity against Herpes B virus 24105 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs	[PMID: 17438061]
Vero	EC₅₀	3.4 μM Compound: TFT	Antiviral activity against Herpes B virus 32425 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs Antiviral activity against Herpes B virus 32425 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs	[PMID: 17438061]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 70-00-8
Appearance Solid
Molecular Weight 296.20
Formel C₁₀H₁₁F₃N₂O₅
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
Synonyms

Trifluorothymidine; 5-Trifluorothymidine; TFT
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
PLoS Pathog

Anti-orthopoxvirus drugs inhibit lumpy skin disease virus replication by targeting viral DNA polymerase. [Abstract]

2026 Jan 26;22(1):e1013903. PMID: 41587213

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3761 mL

16.8805 mL

33.7610 mL

5 mM

0.6752 mL

3.3761 mL

6.7522 mL

10 mM

0.3376 mL

1.6880 mL

3.3761 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Okayama T, et al. Involvement of concentrative nucleoside transporter 1 in intestinal absorption of trifluorothymidine, a novel antitumor nucleoside, in rats. J Pharmacol Exp Ther. 2012 Feb;340(2):457-62. [Content Brief]

[2]. Jia HJ, et al. Trifluridine induces HUVECs senescence by inhibiting mTOR-dependent autophagy. Biochem Biophys Res Commun. 2022 Jun 25;610:119-126. [Content Brief]

[3]. Suzuki N,et al. Trifluridine/tipiracil increases survival rates in peritoneal dissemination mouse models of human colorectal and gastric cancer. Oncol Lett. 2017 Jul;14(1):639-646. [Content Brief]

[4]. Li J, et al. Trifluridine selectively inhibits cell growth and induces cell apoptosis of triple-negative breast cancer. Am J Cancer Res. 2020 Feb 1;10(2):507-522. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Trifluridine

3 Cited Publications

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Trifluridine

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Publications Citing Use of MedChemExpress (MCE) Trifluridine

Alle HSV Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Trifluridine Related Classifications

HY-A0061 Related Classifications