- Tipiracil
-
- $0.00 / 1Kg/Bag
-
2026-04-14
- CAS:183204-72-0
- Min. Order: 1KG
- Purity: 99.5%min HPLC
- Supply Ability: 10kgs
- Tipiracil
-
- $0.00 / 1kg
-
2025-04-04
- CAS:183204-72-0
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1Ton
|
| | Tipiracil hydrochloride Basic information |
| Product Name: | Tipiracil hydrochloride | | Synonyms: | 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;Tipiracil hydrochloride(TPI) | | CAS: | 183204-72-0 | | MF: | C9H12Cl2N4O2 | | MW: | 279.12318 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 183204-72-0.mol |  |
| | Tipiracil hydrochloride Chemical Properties |
| Melting point | 245℃ (decomposition) | | storage temp. | 2-8°C | | solubility | DMSO (Slightly, Heated), Water (Slightly) | | form | powder | | color | white to beige | | Water Solubility | H2O: 5mg/mL, clear (warmed) | | Stability: | Hygroscopic | | InChI | InChI=1S/C9H11ClN4O2.ClH/c10-7-5(12-9(16)13-8(7)15)4-14-3-1-2-6(14)11;/h11H,1-4H2,(H2,12,13,15,16);1H | | InChIKey | KGHYQYACJRXCAT-UHFFFAOYSA-N | | SMILES | C1(=O)NC(CN2CCCC2=N)=C(Cl)C(=O)N1.[H]Cl |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | Tipiracil hydrochloride 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: Tipiracil hydrochloride is 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. It has a role as an antineoplastic agent and an EC 2.4.2.4 (thymidine phosphorylase) inhibitor. It is a hydrochloride and an iminium salt. It contains a tipiracil(1+). | | 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. | | target | thymidine phosphorylase | | References | [1] MASAKAZU FUKUSHIMA . Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2′-deoxyribonucleosides[J]. Biochemical pharmacology, 2000, 59 10: Pages 1227-1236. DOI:10.1016/S0006-2952(00)00253-7.
[2] Kim, Y., Wower, J., Maltseva, N.I., et al. Tipiracil binds to uridine site and inhibits Nsp15 endoribonuclease NendoU from SARS-CoV-2. Commun. Biol. 4(1), 193 (2021).
[3] HIROSHI TSUKIHARA. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts.[J]. Oncology reports, 2015, 33 5: 2135-2142. DOI:10.3892/or.2015.3876.
[4] D L DEXTER. The clinical pharmacology of 5-trifluoromethyl-2’-deoxyuridine.[J]. Cancer research, 1972, 32 2: 247-253. |
| | Tipiracil hydrochloride Preparation Products And Raw materials |
|