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[CAS NO. 183204-74-2]  Tipiracil

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PRODUCTS SPECIFICATIONS [183204-74-2]

Catalog
HY-A0063A
Brand
MCE
CAS
183204-74-2

DESCRIPTION [183204-74-2]

Overview

MDL-
Molecular Weight242.66
Molecular FormulaC9H11ClN4O2
SMILESO=C1NC(C(Cl)=C(CN2C(CCC2)=N)N1)=O

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

4 Publications Citing Use of MCE


Summary

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04854434 Karyopharm Therapeutics Inc
Metastatic Colorectal Cancer
June 29, 2021 Phase 2
NCT03317119 City of Hope Medical Center|National Cancer Institute (NCI)
Metastatic Colon Carcinoma|Metastatic Colorectal Carcinoma|Metastatic Rectal Carcinoma|RAS Family Gene Mutation|Stage III Colon Cancer AJCC v7|Stage III Colorectal Cancer AJCC v7|Stage III Rectal Cancer AJCC v7|Stage IIIA Colon Cancer AJCC v7|Stage IIIA Colorectal Cancer AJCC v7|Stage IIIA Rectal Cancer AJCC v7|Stage IIIB Colon Cancer AJCC v7|Stage IIIB Colorectal Cancer AJCC v7|Stage IIIB Rectal Cancer AJCC v7|Stage IIIC Colon Cancer AJCC v7|Stage IIIC Colorectal Cancer AJCC v7|Stage IIIC Rectal Cancer AJCC v7|Stage IV Colon Cancer AJCC v7|Stage IV Colorectal Cancer AJCC v7|Stage IV Rectal Cancer AJCC v7|Stage IVA Colon Cancer AJCC v7|Stage IVA Colorectal Cancer AJCC v7|Stage IVA Rectal Cancer AJCC v7|Stage IVB Colon Cancer AJCC v7|Stage IVB Colorectal Cancer AJCC v7|Stage IVB Rectal Cancer AJCC v7
April 11, 2018 Phase 1
NCT03981614 Academic and Community Cancer Research United|National Cancer Institute (NCI)
Metastatic Colorectal Carcinoma|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Unresectable Carcinoma
October 29, 2019 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

H 2 O : 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 --- --- ---
10 mM --- --- ---
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

* All of the co-solvents are available by MCE.


Synonyms

2,4(1H,3H)-Pyrimidinedione, 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-
5-Chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione
Tipiracil
TPI (thymidine phosphorylase inhibitor)
MA 1 (pharmaceutical)
MA 1
TPI

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