Tipiracil
Based on 5 publication(s) in Google Scholar
Tipiracil is a thymidine phosphorylase (TPase) inhibitor.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.98%
- CAS 番号: 183204-74-2
- 分子式: C9H11ClN4O2
- 分子量:242.66
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Tipiracil
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生物活性
thymidine phosphorylase[1]
Tipiracil is an inhibitor of thymidine phosphorylase. Tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. The combination of Trifluridine and Tipiracil is a new oral treatment for metastatic colorectal cancer[2]. Tipiracil prevents degradation of FTD through a first-pass effect as a thymidine phosphorylase inhibitor[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 183204-74-2
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性状 Solid
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分子量 242.66
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分子式 C9H11ClN4O2
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Color White to off-white
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SMILES
O=C1NC(C(Cl)=C(CN2C(CCC2)=N)N1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
2021 Jul:139:111672. PMID: 33965731 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Oncol Rep
AZD6738 promotes the tumor suppressive effects of trifluridine in colorectal cancer cells. [Abstract]2023 Mar;49(3):52. PMID: 36734271 -
Mod Rheumatol
Mithramycin has inhibitory effects on gliostatin and matrix metalloproteinase expression induced by gliostatin in rheumatoid fibroblast-like synoviocytes. [Abstract]2018 May;28(3):495-505. PMID: 28741989 -
溶剤 & 溶解度
H2O : 1 mg/mL (4.12 mM; Need ultrasonic)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 2 mg/mL (8.24 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
プロトコル
HeLa cells are seeded in 96-well plates at 500 cells/180 μL/well in triplicate, pre-cultured for 24 h, and then 20 μL of each drug solution is added for 24 or 72 h. For the 24 h treatment, cells are washed with phosphate-buffered saline (PBS) after treatment, drug-free medium is added to each well, and the culture is further incubated for 48 h. Cell growth inhibition is evaluated using a Cell Counting Kit-8. The 50% inhibitory concentration (IC50) values are calculated from the absorbance data using SAS[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
For experiments, 8 mm3 cubic fragments of tumor are implanted subcutaneously into the axilla of mice. For preparation of the orally administered FTD solution, FTD is dissolved in a 0.5% aqueous solution of hydroxypropyl methyl-cellulose (HPMC). The FTD solution for continuous infusion is prepared by dissolving FTD in physiological saline. The TAS-102 dosing solution is composed of FTD and TPI dissolved in a 0.5% aqueous solution of HPMC at a molar ratio of 1:0.5. The dose of TAS-102 is expressed on the basis of the amount of FTD. For preparation of the S-1 solution, FT, CDHP and Oxo are dissolved in a 0.5% aqueous solution of HPMC at a molar ratio of 1:0.4:1. The dose of S-1 is expressed on the basis of the amount of FT. When the tumor volume reaches 100 mm3, the mice are randomly assigned into different treatment groups. Nude mice in the treatment group receive the test compounds. The control group receive no treatment. For continuous infusion, the compound is administered with an osmotic pump. Tumor volume is measured twice a week throughout the experiments. Tumor volume and relative tumor volume are calculated. Body weight changes (BWCs) are used as a proxy measure of side-effects, and calculated. The tumor growth inhibition rate (IR) % on day 15 is used to quantify the antitumor effect.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Lee SJ, et al. Thymidine phosphorylase influences [(18)F]fluorothymidine uptake in cancer cells and patients with non-small cell lung cancer. Eur J Nucl Med Mol Imaging. 2014 Jul;41(7):1327-35. [Content Brief]
[2]. Raedler LA. Lonsurf (Trifluridine plus Tipiracil): A New Oral Treatment Approved for Patients with Metastatic Colorectal Cancer. Am Health Drug Benefits. 2016 Mar;9(Spec Feature):97-100. [Content Brief]
[3]. Tanaka N, et al. Repeated oral dosing of TAS-102 confers high trifluridine incorporation into DNA and sustained antitumor activity in mouse models. Oncol Rep. 2014 Dec;32(6):2319-26. [Content Brief]
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 | 1 mM | 4.1210 mL | 20.6050 mL | 41.2099 mL | 103.0248 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.