Tipiracil hydrochloride
(Synonyms: 盐酸替吡嘧啶) 目录号 : GC14473
A potent TPase inhibitor
Cas No.:183204-72-0
Sample solution is provided at 25 µL, 10mM.
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Tipiracil is an inhibitor of Thymidine phosphorylase (TP).
Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway. It catalyses the reversible phosphorylation of thymidine, and thereby generate thymine and 2-deoxy-D-ribose-1-phosphate.
Tipiracil (TPI) and trifluridine (FTD) are active components of TAS-102 at a molecular ratio of 1:0.5, which is a novel oral nucleoside antitumor agent in clinical trials. Oral administered TPI and FTD co-treatment may differ from that of i.v. administration of FTD alone. [1] When FTD is administered orally, it is rapidly degraded to its inactive form in the intestines and the liver (first-pass effect) [2], but the combination with TPI helps to maintain adequate FTD plasma concentrations [3]. TPI thus, potentiates the antitumor activity of FTD, and the optimal molecular ratio of FTD to TPI has been proven to be 1:0.5. [3]
References:
1. Tsukihara H1, Nakagawa F2, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42.
2. Dexter DL, Wolberg WH, Ansfield FJ, Helson L and Heidelberger C: The clinical pharmacology of 5-trifluoro-methyl-2'-deoxyuridine. Cancer Res 32: 247-253, 1972.
3. Fukushima M, Suzuki N, Emura T et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2'-deoxyribonucleosides. biochem Pharmacol 59: 1227-1236, 2000.
| Animal experiment [1]: | |
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Animal models |
Xenograft-bearing nude mouse models of colorectal and gastric cancers |
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Dosage form |
150 mg/kg/day (combination of Trifluridine and Tipiracil Hydrochloride); p.o.; b.i.d., for 14 days |
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Applications |
The tumor growth-inhibitory activity and RTV5 in mice administered TAS-102 (consisting of Trifluridine and Tipiracil Hydrochloride) with Oxaliplatin were significantly superior to those associated with either monotherapy in mice with colorectal (HCT 116 and SW-48 cells) and gastric (SC-2 and MKN74 cells) cancers. In vivo, TAS-102 alone was effective in MKN74/5FU cells, and its anti-tumor activity was substantially enhanced in combination with Oxaliplatin. No significant decrease in body weight or toxicity was observed compared to either monotherapy. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Tsukihara H, Nakagawa F, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42. | |
| Cas No. | 183204-72-0 | SDF | |
| 别名 | 盐酸替吡嘧啶 | ||
| 化学名 | 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione;hydrochloride | ||
| Canonical SMILES | C1CC(=N)N(C1)CC2=C(C(=O)NC(=O)N2)Cl.Cl | ||
| 分子式 | C9H12Cl2N4O2 | 分子量 | 279.12 |
| 溶解度 | ≥ 13.25 mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5827 mL | 17.9134 mL | 35.8269 mL |
| 5 mM | 0.7165 mL | 3.5827 mL | 7.1654 mL |
| 10 mM | 0.3583 mL | 1.7913 mL | 3.5827 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet