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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Tipiracil HCl (formerly known as TPI; TAS-1-462, MA-1; trade name Lonsurf), the hydrochloride salt of tipiracil, is a thymidine phosphorylase inhibitor (TPI) approved for use in combination (TAS-102) with trifluridine for cancer treatment. One of the active ingredients in TAS-102, which also contains the thymidine phosphorylase inhibitor (TPI) tipiracil and the cytotoxin Trifluridine, is tipiracil. Inhibiting the growth of tumor cells is trifluridine, which is incorporated into DNA during DNA synthesis. When taken orally, tipiracil prevents the breakdown of trifluridine. In 2015, TAS-102 received approval in Japan.
| Targets |
thymidine phosphorylase
|
|---|---|
| ln Vitro |
Tipiracil hydrochloride suppresses the growth of endothelial cells and possesses anti-angiogenic properties [1]. FTD is broken down by the strong thymidine phosphorylase enzyme found in tipiracil hydrochloride [2].
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| References | |
| Additional Infomation |
Tipiracil hydrochloride is a hydrochloride obtained by combining tipiracil with one equivalent of hydrochloric acid. Used in combination with trifluridine, a nucleoside metabolic inhibitor, for treatment of advanced/relapsed unresectable colorectal cancer. It has a role as an antineoplastic agent and an EC 2.4.2.4 (thymidine phosphorylase) inhibitor. It is a hydrochloride and an iminium salt. It contains a tipiracil(1+).
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| Molecular Formula |
C9H12CL2N4O2
|
|---|---|
| Molecular Weight |
279.12318
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| Exact Mass |
278.033
|
| Elemental Analysis |
C, 38.73; H, 4.33; Cl, 25.40; N, 20.07; O, 11.46
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| CAS # |
183204-72-0
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| Related CAS # |
Trifluridine/tipiracil hydrochloride mixture;733030-01-8;Tipiracil;183204-74-2
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| PubChem CID |
9903778
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| Appearance |
White to off-white solid powder
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| LogP |
1.953
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
17
|
| Complexity |
404
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C(N([H])C(N([H])C=1C([H])([H])N1/C(/C([H])([H])C([H])([H])C1([H])[H])=N/[H])=O)=O.Cl[H]
|
| InChi Key |
KGHYQYACJRXCAT-UHFFFAOYSA-N
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| InChi Code |
nChI=1S/C9H11ClN4O2.ClH/c10-7-5(12-9(16)13-8(7)15)4-14-3-1-2-6(14)11;/h11H,1-4H2,(H2,12,13,15,16);1H
|
| Chemical Name |
5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione;hydrochloride
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| Synonyms |
Lonsurf; TAS-1-462; MA-1 MA1Tipiracil HCl; TPI; TAS-102; TAS102
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Water: ~56 mg/mL (~200.6 mM)
DMSO: ~16 mg/mL (~57.3 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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 |
| NCT03317119 | Active Recruiting |
Drug: Trametinib Drug: Trifluridine and Tipiracil Hydrochloride |
RAS Family Gene Mutation Metastatic Rectal Carcinoma |
City of Hope Medical Center | April 11, 2018 | Phase 1 |
| NCT03981614 | Active Recruiting |
Drug: Binimetinib Drug: Palbociclib |
Unresectable Carcinoma Metastatic Colorectal Carcinoma |
Academic and Community Cancer Research United |
October 29, 2019 | Phase 2 |
| NCT04097028 | Active Recruiting |
Drug: Oxaliplatin Drug: Trifluridine and Tipiracil Hydrochloride |
Clinical Stage IIA Esophageal Adenocarcinoma AJCC v8 |
Roswell Park Cancer Institute | December 20, 2019 | Phase 2 |
| NCT04109924 | Active Recruiting |
Drug: Irinotecan Biological: Bevacizumab |
Stage III Colon Cancer AJCC v8 Stage III Colorectal Cancer AJCCv8 |
Roswell Park Cancer Institute | December 27, 2019 | Phase 2 |
| NCT04294264 | Active Recruiting |
Drug: Oxaliplatin Drug: Trifluridine and Tipiracil Hydrochloride |
Stage IV Colon Cancer AJCC v7 Recurrent Colon Carcinoma |
Rutgers, The State University of New Jersey |
February 12, 2019 | Phase 2 |
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