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MedKoo Cat#: 206038 | Name: Trifluridine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Trifluridine (also called trifluorothymidine or TFT) is an anti-herpesvirus antiviral drug, used primarily on the eye. It was sold under the trade name, Viroptic, by Glaxo Wellcome, now merged into GlaxoSmithKline. The brand is now owned by Monarch Pharmaceuticals, which is wholly owned by King Pharmaceuticals. It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the -CF3 group added to the uracil component blocks base pairing. It is a component of the experimental anti-cancer drug TAS-102.

Chemical Structure

Trifluridine
Trifluridine
CAS#70-00-8

Theoretical Analysis

MedKoo Cat#: 206038

Name: Trifluridine

CAS#: 70-00-8

Chemical Formula: C10H11F3N2O5

Exact Mass: 296.0620

Molecular Weight: 296.20

Elemental Analysis: C, 40.55; H, 3.74; F, 19.24; N, 9.46; O, 27.01

Price and Availability

Size Price Availability Quantity
200mg USD 150.00 Ready to ship
500mg USD 300.00 Ready to ship
1g USD 550.00 Ready to ship
2g USD 950.00 Ready to ship
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Related CAS #
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Synonym
FTD ; NSC 529182; NSC-529182; NSC529182; NSC 75520; NSC-75520; NSC75520; Trifluorothymidine; Viroptic; 2-Deoxy-5-trifluoromethyluridine; Trifluridine; 5-Trifluorothymidine;
IUPAC/Chemical Name
1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dione.
InChi Key
VSQQQLOSPVPRAZ-RRKCRQDMSA-N
InChi Code
InChI=1S/C10H11F3N2O5/c11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7/h2,5-7,16-17H,1,3H2,(H,14,18,19)/t5-,6+,7+/m0/s1
SMILES Code
O=C1NC(C(C(F)(F)F)=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
        
Biological target:
Trifluridine is an irreversible thymidylate synthase inhibitor.
In vitro activity:
The cytotoxic effect of trifluridine/tipiracil (FTD/TPI) or oxaliplatin alone or in combination was tested in vitro on murine colon carcinoma CT26 cells (MSS and Kras-mutant cell line). Both viability (crystal violet staining) and cell death (Annexin-V/DAPI labeling) assays showed a synergistic effect for the FTD/TPI and oxaliplatin combination after 24 hours of treatment. Treatment with FTD/TPI alone induced expression of all immunogenic cell death (ICD) markers in CT26 cells at 5 or 50 μmol/L, except for Ifnα1 and Cxcl9 mRNA expression (Fig. 1). In contrast, oxaliplatin alone induced ICD only at 50 μmol/L (Fig. 1). The combination of the drugs was synergistic and significantly enhanced ICD induction as compared with control or monotherapies (Fig. 1). Reference: Cancer Immunol Res. 2019 Dec;7(12):1958-1969. https://cancerimmunolres.aacrjournals.org/content/7/12/1958.long
In vivo activity:
The in vivo capacity of the drugs to induce ICD and thus act on tumor growth by this mechanism was assessed by treating CT26 tumor–bearing mice with FTD/TPI or oxaliplatin alone or the combination of the two drugs. Only the combination of FTD/TPI and oxaliplatin was able to induce HMGB1 cytoplasmic relocalization, similar to that observed after treatment with doxorubicin, used as a positive control (Fig. 3A and B). Similarly, only the FTD/TPI plus oxaliplatin combination induced the phosphorylation of the reticulum stress marker EIF2α in vivo (Fig. 3C and D). A comparison of tumor growth in immunodeficient and immunocompetent mice showed that the antitumor effect only occurred in immunocompetent mice with higher activity of the combination therapy. Despite the absence of HMGB1 cytoplasmic relocalization and EIF2α activation, FTD/TPI or oxaliplatin monotherapy had an antitumor effect in immunocompetent mice. These observations suggest an ICD-independent immune effect, such as depletion of an immunosuppressive population by FTD/TPI or oxaliplatin (Fig. 3E and F). Reference: Cancer Immunol Res. 2019 Dec;7(12):1958-1969. https://cancerimmunolres.aacrjournals.org/content/7/12/1958.long
Solvent mg/mL mM
Solubility
DMSO 56.3 190.18
Water 59.0 199.19
Ethanol 59.0 199.19
DMF 16.0 54.02
PBS (pH 7.2) 5.0 16.88
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 296.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Limagne E, Thibaudin M, Nuttin L, Spill A, Derangère V, Fumet JD, Amellal N, Peranzoni E, Cattan V, Ghiringhelli F. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019 Dec;7(12):1958-1969. doi: 10.1158/2326-6066.CIR-19-0228. Epub 2019 Oct 14. PMID: 31611243.
In vitro protocol:
1. Limagne E, Thibaudin M, Nuttin L, Spill A, Derangère V, Fumet JD, Amellal N, Peranzoni E, Cattan V, Ghiringhelli F. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019 Dec;7(12):1958-1969. doi: 10.1158/2326-6066.CIR-19-0228. Epub 2019 Oct 14. PMID: 31611243.
In vivo protocol:
1. Limagne E, Thibaudin M, Nuttin L, Spill A, Derangère V, Fumet JD, Amellal N, Peranzoni E, Cattan V, Ghiringhelli F. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019 Dec;7(12):1958-1969. doi: 10.1158/2326-6066.CIR-19-0228. Epub 2019 Oct 14. PMID: 31611243.
1: Unseld M, Kühberger S, Graf R, Beichler C, Braun M, Dandachi N, Heitzer E, Prager GW. Circulating tumor DNA (ctDNA) trajectories predict survival in trifluridine/tipiracil-treated metastatic colorectal cancer patients. Mol Oncol. 2025 Jan 22. doi: 10.1002/1878-0261.13755. Epub ahead of print. PMID: 39840713. 2: Thibaudin M, Roussot N, Burlot C, Schmitt A, Vincent J, Tharin Z, Bengrine L, Bellio H, Bertaut A, Hampe L, Daumoine S, Rederstorff E, Peroz M, Huppe T, Derangère V, Rageot D, Simard J, Truntzer C, Fumet JD, Ghiringhelli F. Safety and efficacy of trifluridine/tipiracil +/- bevacizumab plus XB2001 (anti-IL-1α antibody): a single-center phase 1 trial. Signal Transduct Target Ther. 2025 Jan 17;10(1):22. doi: 10.1038/s41392-024-02116-4. PMID: 39820336; PMCID: PMC11739593. 3: Taieb J, Fakih M, Tabernero J, Ciardiello F, Van Cutsem E, Soler G, Calleja E, Barboux V, Roby L, Amellal N, Prager GW. Impact of Treatment With Trifluridine/Tipiracil in Combination With Bevacizumab on Health-Related Quality of Life and Performance Status in Refractory Metastatic Colorectal Cancer: An Analysis of the Phase III SUNLIGHT Trial. Clin Colorectal Cancer. 2024 Dec 11:S1533-0028(24)00116-6. doi: 10.1016/j.clcc.2024.12.002. Epub ahead of print. PMID: 39818468. 4: Jácome AA, Mathias-Machado MC, Gil M, Passarini TM, Cristofaro S, Moraes ED, Freitas LVW, Prolla G, Amorim LC, Paes RD, Gasparotto B, Canedo J, Ferreira CG, Ferrari B, Garicochea B, Gil R, Peixoto RD. Later lines of systemic therapy in patients with metastatic colorectal cancer: real-world data from a setting with barriers to access cancer therapies. J Gastrointest Oncol. 2024 Dec 31;15(6):2543-2551. doi: 10.21037/jgo-24-524. Epub 2024 Dec 28. PMID: 39816030; PMCID: PMC11732344. 5: Lam KO, Li KH, Leung RC, Tang V, Yau T. Trifluridine/Tipiracil (FTD/TPI) in Metastatic Colorectal Cancer in Hong Kong: A Territory-Wide Cohort Study. Adv Ther. 2025 Jan 13. doi: 10.1007/s12325-024-03077-4. Epub ahead of print. PMID: 39804541. 6: Omori Y, Matsukuma S, Kawa M, Ishimitsu K, Kawaoka T, Akiyama N, Tokuno K, Fujita Y, Sato S, Yamamoto S. Prognostic impact and risk factors of severe neutropenia in the early phase of treatment with trifluridine-tipiracil for metastatic colorectal cancer patients: a single-center retrospective study. Int J Colorectal Dis. 2025 Jan 13;40(1):11. doi: 10.1007/s00384-024-04798-2. PMID: 39800823; PMCID: PMC11725538. 7: Ros J, Ucha JM, Garcia-Galea E, Gomez P, Martini G, Balconi F, Comas R, Alonso V, Rodriguez M, Baraibar I, Salva F, Saoudi N, Alcaraz A, Garcia A, Tabernero J, Elez E. Real-World Data of Patients with BRAF V600E-Mutated Metastatic Colorectal Cancer Treated with Trifluridine/Tipiracil. Cancers (Basel). 2024 Dec 12;16(24):4140. doi: 10.3390/cancers16244140. PMID: 39766040; PMCID: PMC11674344. 8: Yamaguchi K, Tsuchihashi K, Ueno S, Uehara K, Taguchi R, Ito M, Isobe T, Imajima T, Kitazono T, Tanoue K, Ohmura H, Akashi K, Baba E. Efficacy of pembrolizumab in microsatellite-stable, tumor mutational burden-high metastatic colorectal cancer: genomic signatures and clinical outcomes. ESMO Open. 2025 Jan 6;10(1):104108. doi: 10.1016/j.esmoop.2024.104108. Epub ahead of print. PMID: 39765187. 9: Takahashi T, Shigeyasu K, Kondo Y, Takeda S, Umeda H, Moriwake K, Kayano M, Sakurai Y, Nakamura S, Takahashi M, Nitta K, Yoshida K, Matsumi Y, Michiue H, Yamamoto H, Kishimoto H, Teraishi F, Shoji R, Kanaya N, Kashima H, Kakiuchi Y, Kuroda S, Kagawa S, Fujiwara T. Predictive marker for response to trifluridine/tipiracil plus bevacizumab in metastatic colorectal cancer patients. BMC Cancer. 2025 Jan 2;25(1):1. doi: 10.1186/s12885-024-13370-8. PMID: 39748254; PMCID: PMC11694457. 10: Shibutani M, Tanda H, Kasashima H, Fukuoka T, Kashiwagi S, Maeda K. Renal impairment as a risk factor for chemotherapy induced neutropenia in the treatment of trifluridine/thymidine phosphorylase inhibitor plus bevacizumab. Sci Rep. 2025 Jan 2;15(1):553. doi: 10.1038/s41598-024-84133-5. PMID: 39747494; PMCID: PMC11696094. 11: Signorelli C, Calegari MA, Anghelone A, Passardi A, Frassineti GL, Bittoni A, Lucchetti J, Angotti L, Di Giacomo E, Zurlo IV, Morelli C, Dell'Aquila E, Artemi A, Gemma D, Corsi DC, Emiliani A, Ribelli M, Mazzuca F, Arrivi G, Zoratto F, Chilelli MG, Schirripa M, Morandi MG, Santamaria F, Dettori M, Cosimati A, Saltarelli R, Minelli A, Lucci-Cordisco E, Basso M. Survival Outcomes with Regorafenib and/or Trifluridine/Tipiracil Sequencing to Rechallenge with Third- Line Regimens in Metastatic Colorectal Cancer: A Multicenter Retrospective Real- World Subgroup Comparison from the ReTrITA Study. Curr Oncol. 2024 Dec 4;31(12):7793-7808. doi: 10.3390/curroncol31120574. PMID: 39727697; PMCID: PMC11674570. 12: Lin R, Cheng J, Zhao J, Zhou L, Li J, Yang X. Anticancer effects of PEP06 (TB01) in combination with Trifluridine/Tipiracil (TAS-102) in a xenograft model of human colorectal cancer. J Cancer Res Clin Oncol. 2024 Dec 26;151(1):22. doi: 10.1007/s00432-024-05984-z. PMID: 39724415; PMCID: PMC11671547. 13: Wu C, Li S, Hou X. A real-world study: third-line treatment options for metastatic colorectal cancer. Front Oncol. 2024 Dec 2;14:1480704. doi: 10.3389/fonc.2024.1480704. PMID: 39687893; PMCID: PMC11648419. 14: Huang J, Gao Y, Liu J, Yang Z, Zhang X. System biology analysis of miRNA- gene interaction network reveals novel drug targets in breast cancer. Nucleosides Nucleotides Nucleic Acids. 2024 Dec 4:1-16. doi: 10.1080/15257770.2024.2436421. Epub ahead of print. PMID: 39630693. 15: Tseng KY, Yang MY, Chen WS, Jiang JK, Wang HS, Chang SC, Lan YT, Lin CC, Lin HH, Huang SC, Cheng HH, Yang YW, Lin YZ, Chang CY, Teng HW. Combining moderate dosage of Bevacizumab with TAS-102 provides longer progression-free time in refractory metastatic colorectal Cancer. Int J Colorectal Dis. 2024 Dec 4;39(1):195. doi: 10.1007/s00384-024-04767-9. PMID: 39630293; PMCID: PMC11618181. 16: Huang LZ, Chen YQ, Gu HY, Chen Y. Cost-effectiveness analysis of trifluridine/tipiracil combined with bevacizumab vs. monotherapy for third-line treatment of colorectal cancer. Front Public Health. 2024 Nov 13;12:1465898. doi: 10.3389/fpubh.2024.1465898. PMID: 39606076; PMCID: PMC11599266. 17: Sarti K, Boige V, Camilleri GM, Ducreux M, Boilève A. Defying the odds: Outstanding survival in lung-only pancreatic cancer treated by Trifluridine- Tipiracil. Eur J Cancer. 2025 Jan;214:115125. doi: 10.1016/j.ejca.2024.115125. Epub 2024 Nov 14. PMID: 39578184. 18: Chang YW, Kuo CN, Chang CL, Hsu JC, Ko Y. Effectiveness and Safety of Regorafenib and TAS-102 in Patients with Metastatic Colorectal Cancer: A Nationwide Population-Based Study in Taiwan. Cancer Res Treat. 2024 Nov 18. doi: 10.4143/crt.2024.376. Epub ahead of print. PMID: 39563201. 19: Ciracì P, Studiale V, Taravella A, Antoniotti C, Cremolini C. Late-line options for patients with metastatic colorectal cancer: a review and evidence- based algorithm. Nat Rev Clin Oncol. 2025 Jan;22(1):28-45. doi: 10.1038/s41571-024-00965-0. Epub 2024 Nov 18. PMID: 39558030. 20: Fumet JD, Roussot N, Bertaut A, Limagne E, Thibaudin M, Hervieu A, Zanetta S, Borg C, Senellart H, Pernot S, Thuillier F, Carnot A, Mineur L, Chibaudel B, Touchefeu Y, Martin-Babau J, Jary M, Labourey JL, Rederstorff E, Lepage C, Ghiringhelli F. Phase I/II study of trifluridine/tipiracil plus XB2001 versus trifluridine/tipiracil in metastatic colorectal cancer. Future Oncol. 2024;20(38):3077-3085. doi: 10.1080/14796694.2024.2415280. Epub 2024 Nov 12. PMID: 39530624.