Trifluridine/tipiracil hydrochloride mixture
Based on 4 publication(s) in Google Scholar
Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA.
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- 純度: 99.96%
- CAS 番号: 733030-01-8
- 分子式: C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl
- 分子量:435.76
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Trifluridine/tipiracil hydrochloride mixture
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
生物活性
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude mice bearing KM12C, KM12C/5-FU, DLD-1, DLD-1/5-FU, and SC-2 cells[2]
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Dosage:150 mg/kg/day
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Administration:p.o.; twice a day for 14 days
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Result:Prevented body weight loss and reduced the relative tumor volume in colorectal cancer and gastric cancer mice models.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 733030-01-8
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性状 Solid
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分子量 435.76
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分子式 C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl
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Color White to off-white
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SMILES
O=C1N([C@H]2C[C@H](O)[C@@H](CO)O2)C=C(C(F)(F)F)C(N1)=O.O=C3NC(CN4CCCC4=N)=C(Cl)C(N3)=O.[1/2].Cl
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別名
TAS-102; FTD/TPI
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Transl Oncol
A CEBPB/TYMP/GDF15 signaling axis mediates tumor growth and cisplatin resistance in bladder cancer. [Abstract]2025 Nov:61:102537. PMID: 40957398
Trifluridine/tipiracil hydrochloride mixture purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Nov:61:102537. [Abstract]
Cell viability of UMUC3 cells treated with Trifluridine/tipiracil hydrochloride mixture (TAS-102, 20 μM) or DMSO.
Trifluridine/tipiracil hydrochloride mixture purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Nov:61:102537. [Abstract]
In vivo tumor growth in C57BL/6 mice bearing MB49 xenografts treated with PBS, cisplatin, Trifluridine/tipiracil hydrochloride mixture (TAS-102, 20 mg/kg, ip, twice a week), or both (C + T); representative tumor images are shown.
Trifluridine/tipiracil hydrochloride mixture purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Nov:61:102537. [Abstract]
In vivo tumor growth in C57BL/6 mice bearing MB49 xenografts treated with PBS, cisplatin, Trifluridine/tipiracil hydrochloride mixture (TAS-102, 20 mg/kg, ip, twice a week), or both (C + T); representative tumor weight are shown.
Trifluridine/tipiracil hydrochloride mixture purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Nov:61:102537. [Abstract]
In vivo tumor growth in C57BL/6 mice bearing MB49 xenografts treated with PBS, cisplatin, Trifluridine/tipiracil hydrochloride mixture (TAS-102, 20 mg/kg, ip, twice a week), or both (C + T); representative tumor volume are shown.
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Am J Cancer Res
2020 Nov 1;10(11):3752-3764. PMID: 33294265 -
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bioRxiv
BOGO: A Proteome-Wide Gene Overexpression Platform for Discovering Rational Cancer Combination Therapies. [Abstract]2025 Sep 7:2025.09.02.673780. PMID: 40950237
溶剤 & 溶解度
H2O : 100 mg/mL (229.48 mM; Need ultrasonic)
DMSO : 50 mg/mL (114.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 20 mg/mL (45.90 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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: 50 mg/mL (114.74 mM); Clear solution; Need ultrasonic
Add each solvent one by one: Saline
Solubility: 100 mg/mL (229.48 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Emura T, et al. A novel antimetabolite, TAS-102 retains its effect on FU-related resistant cancer cells. Int J Mol Med. 2004;13(4):545-549. [Content Brief]
[2]. Nukatsuka M, et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts. Anticancer Res. 2015;35(3):1437-1445. [Content Brief]
[3]. Limagne E, Thibaudin M, Nuttin L, et al. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019;7(12):1958-1969. [Content Brief]
[4]. Suzuki N, Nakagawa F, Takechi T. Trifluridine/tipiracil increases survival rates in peritoneal dissemination mouse models of human colorectal and gastric cancer [published correction appears in Oncol Lett. 2021 Jul;22(1):511]. Oncol Lett. 2017;14(1):639-646. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMF / DMSO / H2O | 1 mM | 2.2948 mL | 11.4742 mL | 22.9484 mL | 57.3710 mL |
| 5 mM | 0.4590 mL | 2.2948 mL | 4.5897 mL | 11.4742 mL | |
| 10 mM | 0.2295 mL | 1.1474 mL | 2.2948 mL | 5.7371 mL | |
| 15 mM | 0.1530 mL | 0.7649 mL | 1.5299 mL | 3.8247 mL | |
| 20 mM | 0.1147 mL | 0.5737 mL | 1.1474 mL | 2.8686 mL | |
| 25 mM | 0.0918 mL | 0.4590 mL | 0.9179 mL | 2.2948 mL | |
| 30 mM | 0.0765 mL | 0.3825 mL | 0.7649 mL | 1.9124 mL | |
| 40 mM | 0.0574 mL | 0.2869 mL | 0.5737 mL | 1.4343 mL | |
| DMSO / H2O | 50 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1474 mL |
| 60 mM | 0.0382 mL | 0.1912 mL | 0.3825 mL | 0.9562 mL | |
| 80 mM | 0.0287 mL | 0.1434 mL | 0.2869 mL | 0.7171 mL | |
| 100 mM | 0.0229 mL | 0.1147 mL | 0.2295 mL | 0.5737 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/tipiracil hydrochloride mixture 関連分類
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