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| Tipiracil Basic information |
| Product Name: | Tipiracil | | Synonyms: | Tipiracil;Tipiracil (hydrochloride);2,4(1H,3H)-PyriMidinedione,5-chloro-6-[(2-iMino-1-pyrrolidinyl)Methyl] hydrochloride;5-Chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione monohydrochloride;Tipiracil HCl;5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,hydrochloride;5-Chloro-6-(2-iminopyrrolidin-1-ylmethyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione hydrochloride;5-Chloro-6-(2-iminopyrrolidin-1-ylmethyl)uracil hydrochloride | | CAS: | 183204-72-0 | | MF: | C9H12Cl2N4O2 | | MW: | 279.12318 | | EINECS: | | Product Categories: | Inhibitors;API | | Mol File: | 183204-72-0.mol |
| Tipiracil Chemical Properties |
| Melting point | 245℃ (decomposition) | | storage temp. | 2-8°C | | solubility | DMSO (Slightly, Heated), Water (Slightly) | | form | powder | | color | white to beige | | Stability: | Hygroscopic |
| Tipiracil Usage And Synthesis |
| Description | Tipiracil (TPI) is a potent and competitive inhibitor of thymidine phosphorylase (TPase) with an IC50 value of 35 nM for human placental TPase. 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 , 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. | | Uses | Tipiracil Hydrochloride serves as a treatment for metastatic colorectal cancer (mCRC). A thymidine phosphorylase inhibitor. | | Definition | ChEBI: A hydrochloride obtained by combining tipiracil with one equivalent of hydrochloric acid. Used in combination with trifluridine, a nucleoside metabolic inhibitor, for treatment of advanced/relapsed unresectable colorectal cancer. | | 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. |
| Tipiracil Preparation Products And Raw materials |
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