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| 100mg |
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| 250mg |
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Tipiracil (TPI), one of the main ingredients in TAS-102 (trade name Lonsurf, a mixture of Trifluridine and tipiracil hydrochloride in a 1:0.5 molar ratio), is a potent thymidine phosphorylase (TPase) inhibitor with anticancer activity. TAS-102 has been approved in Japan in 2015.
| Targets |
thymidine phosphorylase
|
|---|---|
| ln Vitro |
Thymidine phosphorylase is inhibited by the drug tipiracil. Tipiracil increases trifluridine exposure by preventing thymidine phosphorylase from metabolizing the drug. A brand-new oral treatment for metastatic colorectal cancer combines trifluridine and piracil[2]. As a thymidine phosphorylase inhibitor, tipiracil has a first-pass effect that prevents FTD from degrading[3].
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| Cell Assay |
HeLa cells are plated in triplicate in 96-well plates at a density of 500 cells/180 μL/well and pre-cultured for 24 hours before receiving 20 μL of each drug solution for 24 or 72 hours. Following the 24 h treatment, cells are washed with phosphate-buffered saline (PBS) before being added to each well with drug-free medium and being incubated for an additional 48 h. A Cell Counting Kit-8 is used to assess the inhibition of cell growth. SAS[3] is used to determine the 50% inhibitory concentration (IC50) values from the absorbance data.
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| References |
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| Molecular Formula |
C9H11N4O2CL
|
|---|---|
| Molecular Weight |
242.66224
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| Exact Mass |
242.0570533
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| CAS # |
183204-74-2
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| Related CAS # |
Trifluridine/tipiracil hydrochloride mixture;733030-01-8;Tipiracil hydrochloride;183204-72-0
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| Appearance |
Solid
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| SMILES |
C1CC(=N)N(C1)CC2=C(C(=O)NC(=O)N2)Cl
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| InChi Key |
QQHMKNYGKVVGCZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H11ClN4O2/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)
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| Chemical Name |
5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione
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| Synonyms |
Tipiracil
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
H2O: ~1 mg/mL (~4.1 mM)
DMSO: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (8.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1210 mL | 20.6050 mL | 41.2099 mL | |
| 5 mM | 0.8242 mL | 4.1210 mL | 8.2420 mL | |
| 10 mM | 0.4121 mL | 2.0605 mL | 4.1210 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 |
| NCT04737187 | Active Recruiting |
Drug: Bevacizumab | Refractory Metastatic Colorectal Cancer |
Taiho Oncology, Inc. | November 25, 2020 | Phase 3 |
| 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 |
| NCT03981614 | Active Recruiting |
Drug: Binimetinib Drug: Palbociclib |
Unresectable Carcinoma Metastatic Colorectal Carcinoma |
Academic and Community Cancer Research United |
October 29, 2019 | Phase 2 |
| NCT05198934 | Active Recruiting |
Drug: Sotorasib Drug: Panitumumab |
Colorectal Cancer (CRC) | Amgen | April 19, 2022 | Phase 3 |
| NCT03317119 | Active Recruiting |
Drug: Trametinib Drug: Trifluridine and Tipiracil Hydrochloride |
RAS Family Gene Mutation Metastatic Colon Carcinoma |
City of Hope Medical Center |
April 11, 2018/td> | Phase 1 |
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