183204-72-0 Usage
Description
Tipiracil (TPI) is a potent and selective inhibitor of thymidine phosphorylase (TPase), a key enzyme involved in the metabolism of pyrimidine nucleosides. With an IC50 value of 35 nM for human placental TPase, TPI effectively inhibits the phosphorolysis and degradation of trifluorothymidine, a cytotoxic nucleoside, in human breast and colon carcinoma tumor samples. It is used in combination with trifluridine, a nucleoside metabolic inhibitor, for the treatment of advanced or relapsed unresectable colorectal cancer.
Uses
Used in Pharmaceutical Industry:
Tipiracil is used as an anticancer agent for the treatment of metastatic colorectal cancer (mCRC). It functions as a thymidine phosphorylase inhibitor, enhancing the anti-tumor activity of trifluorothymidine when administered orally in a mouse AZ-521 stomach cancer xenograft model. Formulations containing TPI have been specifically developed for this application, targeting the inhibition of TPase and improving the efficacy of trifluorothymidine in cancer treatment.
Biochem/physiol Actions
Tipiracil is an inhibitor of thymidine phosphorylase. Tipiracil is used in combination with trifluridine as TAS-102 for the treatment of refractory metastatic colorectal cancer. Tipiracil increases the bioavailability of trifluridine by blocking the enzyme that would otherwise protect the tumors by metabolizing trifluridine.
references
1. tsukihara h1, nakagawa f2, sakamoto k et al. efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, tas-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. oncol rep. 2015 may;33(5):2135-42. 2. dexter dl, wolberg wh, ansfield fj, helson l and heidelberger c: the clinical pharmacology of 5-trifluoro-methyl-2'-deoxyuridine. cancer res 32: 247-253, 1972.3. fukushima m, suzuki n, emura t et al. structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2'-deoxyribonucleosides. biochem pharmacol 59: 1227-1236, 2000.
Check Digit Verification of cas no
The CAS Registry Mumber 183204-72-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,3,2,0 and 4 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 183204-72:
(8*1)+(7*8)+(6*3)+(5*2)+(4*0)+(3*4)+(2*7)+(1*2)=120
120 % 10 = 0
So 183204-72-0 is a valid CAS Registry Number.
