A potent TPase inhibitor (IC50 = 35 nM for human placental TPase); selective for TPase over other pyrimidine-metabolizing enzymes (IC50s = >1 mM for UPase

Tipiracil (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
183204-72-0
Storage:
-20
UN-No:
Non-Hazardous - /

Tipiracil (TPI) is a potent and competitive inhibitor of thymidine phosphorylase (TPase) with an IC50 value of 35 nM for human placental TPase.{40279} It is selective for TPase over other pyrimidine-metabolizing enzymes (IC50s = >1 mM for UPase, OPRTase, TK, and DPDase). TPI inhibits the phosphorolysis and degradation of trifluorothymidine (Item No. 21366), a cytotoxic nucleoside, in human breast and colon carcinoma tumor samples. Oral administration of TPI (12.5-50 mg/kg) enhances the anti-tumor activity of trifluorothymidine in a mouse AZ-521 stomach cancer xenograft model. Formulations containing TPI have been used for the treatment of metastatic colorectal cancer.{40281}  

 

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Description

A potent TPase inhibitor (IC50 = 35 nM for human placental TPase); selective for TPase over other pyrimidine-metabolizing enzymes (IC50s = >1 mM for UPase, OPRTase, TK, and DPDase); inhibits the phosphorolysis and degradation of trifluorothymidine in human breast and colon carcinoma tumor samples; enhances anti-tumor activity of trifluorothymidine in a mouse AZ-521 stomach cancer xenograft model

Formal name: 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione, monohydrochloride

Synonyms:  TPI

Molecular weight: 279.1

CAS: 183204-72-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer

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