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Trifluridine
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Catalog No. T1428Cas No. 70-00-8
Alias Viroptic, Trifluridina, Trifluorothymidine, NSC 75520, NSC 529182, 5-Trifluorothymidine
Trifluridine (NSC-75520) is a fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity.
Trifluridine
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Purity: 99.82%
Catalog No. T1428Alias Viroptic, Trifluridina, Trifluorothymidine, NSC 75520, NSC 529182, 5-TrifluorothymidineCas No. 70-00-8
Trifluridine (NSC-75520) is a fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $30 | In Stock | In Stock | |
| 25 mg | $46 | In Stock | In Stock | |
| 50 mg | $65 | In Stock | In Stock | |
| 100 mg | $87 | In Stock | In Stock | |
| 200 mg | $135 | In Stock | In Stock | |
| 500 mg | $223 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $63 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.82%
Color:White
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Product Introduction
Trifluridine AI Summary
Trifluridine demonstrates extensive bioactivity across various biological targets. It exhibits inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis with a Ki value of 97000.0 nM and shows potent inhibition of thymidylate synthase in L1210 cells with ID50 of 0.035 µM. The compound also inhibits [3H]TdR incorporation into DNA in HL-60 cells (ID50 = 14.0 µM), and demonstrates antiviral activity against HSV-1 and HSV-2 with EC50 values in the nanomolar range. Additionally, Trifluridine inhibits the replication of liver cells as well as other virus-induced cytopathogenic effects in several assays.
Its enzyme-related activities include a high Michaelis-Menten constant (Km) of 798,000.0 nM against horse liver thymidine phosphorylase and a Vmax value of 8.53 µM min-1. The compound shows antitumor activity against tumor sarcoma 180 with an effective dose of 63.0 mg kg-1 day-1 and 100% inhibition at 0.1 µM in vitro S-180 cell assays.
Trifluridine shows cytotoxicity against various cell lines: mouse L1210/0 cells (IC50 = 20 nM after 48 hours), human HuH7 cells (CC50 greater than 200.0 µg/mL), and African green monkey Vero cells (CC50 of 50,600 nM). It curtails the uptake of sodium fluorescein in OATP1B1 and OATP1B3-transfected CHO cells, showing inhibitory rates of 64.99% and 84.35%, respectively, at 10 µM.
The compound exhibits selective binding affinities towards multiple human and rat receptors, with AC50 values generally greater than 10,000.0 nM, and impacts various enzymes like PTGS2, MAOA, and PDE3A. Additionally, antiviral activities span across multiple viruses including DHBV, HBV (with EC50 values in the low nanomolar range), and some efficacy against SARS-CoV-2, though with moderate to low potency.
Trifluridine does not exhibit significant liver toxicity and shows no inhibition of human BSEP activity at IC50 greater than 1,000,000.0 nM. These broad-ranging bioactivities suggest that Trifluridine has potential therapeutic applications across various conditions involving cell function, antiviral responses, and tumor cell viability..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Trifluridine (NSC-75520) is a fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity. |
| In vitro | Differences in substrate specificity at TK1 and DUT resulted in substantial Trifluridine (FTD) incorporation into DNA. Trifluridine-treated cells display nuclear morphology compared to 2'-deoxy-5-fluorouridine-treated cells.Trifluridine dose-dependently inhibits the proliferation of human colorectal cancer cells transplanted into nude mice and mouse bone marrow cells.Trifluridine dose-dependently inhibits colony-forming bone marrow cells. |
| In vivo | Differences in substrate specificity at TK1 and DUT resulted in substantial Trifluridine (FTD) incorporation into DNA. Trifluridine-treated cells display nuclear morphology compared to 2'-deoxy-5-fluorouridine-treated cells.Trifluridine dose-dependently inhibits the proliferation of human colorectal cancer cells transplanted into nude mice and mouse bone marrow cells.Trifluridine dose-dependently inhibits colony-forming bone marrow cells. |
| Synonyms | Viroptic, Trifluridina, Trifluorothymidine, NSC 75520, NSC 529182, 5-Trifluorothymidine |
| Molecular Weight | 296.2 |
| Formula | C10H11F3N2O5 |
| Cas No. | 70-00-8 |
| Smiles | O=C1N([C@@H]2O[C@H](CO)[C@@H](O)C2)C=C(C(F)(F)F)C(=O)N1 |
| Relative Density. | 1.646g/cm3 |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 14.8 mg/mL (49.97 mM), Sonication is recommended. DMSO: 255 mg/mL (860.9 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (16.88 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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