| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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Purity: ≥98%
Tegafur (formerly known as Fluorafur, FT-207, NSC-148958; Uftoral; UFT), a component of tegafur-uracil, is a chemotherapeutic anticancer prodrug of 5-FU (5-Fluorouracil, an anticancer drug) that is commonly used in the treatment of various cancers. Tegafur can become 5-FU when it is metabolized in an in vivo environment. A combination of the 5-fluorouracil (5-FU) congener prodrug tegafur (tetrahydrofuranyl-5-fluorouracil) and uracil (1:4) is used to formulate Tegafur-uracil, a therapeutic oral agent.
| Targets |
Nucleoside antimetabolite/analog
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| ln Vitro |
Tegafur is a bioactivator of the hepatic microsomal cytochrome P450 enzyme, 5-FU. The active metabolites 5-fluorodeoxyuridine-monophosphate (FdUMP) and 5-fluorouridine-triphosphate (FUTP), which are embedded in cells and inhibit thymidylate synthase, are produced intracellularly from 5-FU mask. This leads to decreased thymidine synthesis, decreased DNA synthesis, disruption of RNA function, and toxicity to tumor cells.
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| References |
[1]. Sotaro Sadahiro, Toshiyuki Suzuki, Akira Tanaka, et al. Association of right-sided tumors with high thymidine phosphorylase gene expression levels and the response to oral uracil and tegafur/leucovorin chemotherapy among patients with colorectal cancer. Cancer Chemotherapy and Pharmacology. 2012, 70 (2): 285-291.
[2]. José L. Ariasa, et al. Engineering of an antitumor (core/shell) magnetic nanoformulation based on the chemotherapy agent ftorafur. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2011,384(1-3): 157-163. [3]. Gabriel N. Hortobagyi, William Heim, Laura Hutchins, et al. A phase 2 study of a fixed combination of uracil and ftorafur (UFT) and leucovorin given orally in a 3-times-daily regimen to treat patients with recurrent metastatic breast cancer. Cancer. 2010, 116(6): 1440-1445. [4]. K. Fujita, H. Nakayama, W. Ichikawa, et al. Pharmacokinetics of 5-Fluorouracil in Elderly Japanese Patients with Cancer Treated with S-1 (a Combination of Tegafur and Dihydropyrimidine Dehydrogenase Inhibitor 5-Chloro-2,4-dihydroxypyridine). Drug Metab Dispos. 2009 Jul;37(7):1375-7. doi: 10.1124/dmd.109.027052. Epub 2009 Apr 23. [5]. Tegafur-uracil |
| Molecular Formula |
C8H9FN2O3
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|---|---|---|
| Molecular Weight |
200.17
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| Exact Mass |
200.06
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| Elemental Analysis |
C, 48.00; H, 4.53; F, 9.49; N, 14.00; O, 23.98
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| CAS # |
17902-23-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CC(OC1)N2C=C(C(=O)NC2=O)F
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| InChi Key |
WFWLQNSHRPWKFK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H9FN2O3/c9-5-4-11(6-2-1-3-14-6)8(13)10-7(5)12/h4,6H,1-3H2,(H,10,12,13)
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| Chemical Name |
5-fluoro-1-(oxolan-2-yl)pyrimidine-2,4-dione
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| Synonyms |
Fluorafur; FT-207; NSC-148958; FT207; NSC148958; FT 207; NSC 148958; Uracil; Ftorafur; Uracil; Tegafur; Trade name: Uftoral; UFT.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9958 mL | 24.9788 mL | 49.9575 mL | |
| 5 mM | 0.9992 mL | 4.9958 mL | 9.9915 mL | |
| 10 mM | 0.4996 mL | 2.4979 mL | 4.9958 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04310774 | Not yet recruiting | Drug: Tegafur, Gimeracil and Oteracil Potassium Capsules (one drug) |
Cervical Cancer Chemotherapy |
Peking Union Medical College Hospital |
April 15, 2020 | Phase 2 Phase 1 |
| NCT02836977 | Active Recruiting |
Drug: tegafur-uracil | Stage III Colon Cancer | Kaohsiung Medical University Chung-Ho Memorial Hospital |
March 2016 | Not Applicable |
| NCT00464919 | Completed | Drug: Sorafenib Drug: tegafur/uracil (UFUR®) |
Hepatocellular Carcinoma | National Taiwan University Hospital |
April 2007 | Phase 2 |
| NCT02447679 | Completed | Drug: thalidomine Drug: tegafur-uracil |
Adult Hepatocellular Carcinoma Adverse Reaction to Drug |
Chang Gung Memorial Hospital | August 2010 | Phase 2 |
| NCT01037998 | Completed | Drug: UFUR and Iressa | Non-Small-Cell Lung Cancer | Taipei Veterans General Hospital, Taiwan |
November 2005 | Phase 2 |
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