2. Apoptosis Cell Cycle/DNA Damage
  3. Thymidylate Synthase Nucleoside Antimetabolite/Analog
  4. Tipiracil

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

For research use only. We do not sell to patients.

Tipiracil Chemical Structure

Tipiracil Chemical Structure

CAS No. : 183204-74-2

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Tipiracil:

Tipiracil Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

IC50 & Target

thymidine phosphorylase[1]
In Vitro

Tipiracil is an inhibitor of thymidine phosphorylase. Tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. The combination of Trifluridine and Tipiracil is a new oral treatment for metastatic colorectal cancer[2]. Tipiracil prevents degradation of FTD through a first-pass effect as a thymidine phosphorylase inhibitor[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tipiracil Related Antibodies
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT04511039Roswell Park Cancer Institute|Pfizer
Advanced Malignant Solid Neoplasm|Clinical Stage III Gastroesophageal Junction Adenocarcinoma|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma A|Locally Advanced Colorectal Carcinoma|Locally Advanced Gastroesophageal Junction Adenocarcinoma|Metastatic Colorectal Adenocarcinoma|Metastatic Gastroesophageal Junction Adenocarcinoma|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8
June 8, 2021Phase 1
NCT04854434Karyopharm Therapeutics Inc
Metastatic Colorectal Cancer
June 29, 2021Phase 2
NCT04294264Rutgers, The State University of New Jersey|National Cancer Institute (NCI)
Metastatic Colorectal Carcinoma|Recurrent Colon Carcinoma|Refractory Colorectal Carcinoma|Stage IV Colon Cancer AJCC v7|Stage IVA Colon Cancer AJCC v7|Stage IVB Colon Cancer AJCC v7
February 12, 2019Phase 2
Molecular Weight

242.66

Formula

C9H11ClN4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C(Cl)=C(CN2C(CCC2)=N)N1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 1 mg/mL (4.12 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1210 mL 20.6050 mL 41.2099 mL
5 mM --- --- ---
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 2 mg/mL (8.24 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Purity & Documentation
References
Cell Assay
[3]

HeLa cells are seeded in 96-well plates at 500 cells/180 μL/well in triplicate, pre-cultured for 24 h, and then 20 μL of each drug solution is added for 24 or 72 h. For the 24 h treatment, cells are washed with phosphate-buffered saline (PBS) after treatment, drug-free medium is added to each well, and the culture is further incubated for 48 h. Cell growth inhibition is evaluated using a Cell Counting Kit-8. The 50% inhibitory concentration (IC50) values are calculated from the absorbance data using SAS[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
For experiments, 8 mm3 cubic fragments of tumor are implanted subcutaneously into the axilla of mice. For preparation of the orally administered FTD solution, FTD is dissolved in a 0.5% aqueous solution of hydroxypropyl methyl-cellulose (HPMC). The FTD solution for continuous infusion is prepared by dissolving FTD in physiological saline. The TAS-102 dosing solution is composed of FTD and TPI dissolved in a 0.5% aqueous solution of HPMC at a molar ratio of 1:0.5. The dose of TAS-102 is expressed on the basis of the amount of FTD. For preparation of the S-1 solution, FT, CDHP and Oxo are dissolved in a 0.5% aqueous solution of HPMC at a molar ratio of 1:0.4:1. The dose of S-1 is expressed on the basis of the amount of FT. When the tumor volume reaches 100 mm3, the mice are randomly assigned into different treatment groups. Nude mice in the treatment group receive the test compounds. The control group receive no treatment. For continuous infusion, the compound is administered with an osmotic pump. Tumor volume is measured twice a week throughout the experiments. Tumor volume and relative tumor volume are calculated. Body weight changes (BWCs) are used as a proxy measure of side-effects, and calculated. The tumor growth inhibition rate (IR) % on day 15 is used to quantify the antitumor effect.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 4.1210 mL 20.6050 mL 41.2099 mL 103.0248 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.

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Tipiracil Related Classifications

Keywords:

Tipiracil183204-74-2Thymidylate SynthaseNucleoside Antimetabolite/AnalogInhibitorinhibitorinhibit

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