Tipiracil hydrochloride (Synonyms: TPI) |
| Catalog No.GC14473 |
A potent TPase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | TPI | ||
| Chemical Name | 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 | ||
| Formula | C9H12Cl2N4O2 | M.Wt | 279.12 |
| Solubility | ≥ 13.25 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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