733030-01-8
Tipiracil hydrochloride-trifluridine mixt
CAS: 733030-01-8
Molecular Formula: C10H11F3N2O5. 1/2C9H11ClN4O2.
733030-01-8 - Names and Identifiers
733030-01-8 - Physico-chemical Properties
| Molecular Formula | C10H11F3N2O5. 1/2C9H11ClN4O2. |
| Molar Mass | 435.76 |
| Melting Point | 170-172°C |
| Solubility | DMSO: 2.34 mg/mL (Need ultrasonic and warming) |
| Appearance | Form Solid, color White to Off-White |
| Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
| Stability | Hygroscopic |
| Physical and Chemical Properties | Bioactive TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is a combination of thymidine nucleate analog trifluridine and thymidine phosphatase inhibitor tipiracil hydrochloride for oral administration. |
733030-01-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.295 ml | 11.474 ml | 22.948 ml |
| 5 mM | 0.459 ml | 2.295 ml | 4.59 ml |
| 10 mM | 0.229 ml | 1.147 ml | 2.295 ml |
| 5 mM | 0.046 ml | 0.229 ml | 0.459 ml |
Last Update：2024-01-02 23:10:35
733030-01-8 - Uses and synthesis methods
in vitro studies
TAS-102 is an oral combination drug, including trifluorouridine (FTD, thymidine nucleic acid analog) and dipifolin hydrochloride (TPI, which can inhibit the catabolism of FTD by thymidine phosphorylase, thereby improving the oral biological activity of FTD). The phosphorylation of trifluridine is inserted into DNA, causing DNA dysfunction and cell cycle arrest. Thymidine phosphatase inhibitor (TPI) inhibits FTD degradation and angiogenesis. Therefore, TAS-102 treatment can lead to a large amount of trifluridine being incorporated into DNA, activating a pathway similar to DNA damage reaction, Chk1 phosphorylation and cell arrest in G2/M phase.
In vivo studies
In humans, intravenous injection of TAS-102, the elimination half-life of its component FTD is very short (18 min), and it degrades rapidly in vitro. Its main metabolite is 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione. In monkeys, plasma FTD levels were very low after oral administration of FTD alone, indicating extensive first-pass metabolism of it by liver and intestinal TPse. However, the addition of TPI(tipiracil hydrochloride) can stabilize FTD and improve its oral activity. TPI inhibits the degradation of FTD in liver and intestine after oral administration by inhibiting thymidine phosphorylase. Thymidine phosphorylase (TP) can catalyze pyrimidine 2 & prime;-Phosphorolysis of deoxynucleosides (such as FTD). Studies in mouse models carrying human CRC tumors have shown that the combination achieves maximum antitumor activity when the mixing ratio of FTD to TPI is 1:0.5; studies in mice and monkeys show that the concentration of FTD in plasma reaches maximum at this mixing ratio. In addition, the mixing ratio can make the TAS-102 reach the best balance between anti-tumor activity and toxic effect. In mice, TPI and FTD combined administration had a lower toxic effect than FTP alone. TAS-102 overcomes 5-FU resistance because the main mechanism of action of TAS-102 is independent of the major metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has potent activity in 5-FU-tolerant cancers.
Last Update：2024-04-09 01:59:50
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Product Name: 1-((2R,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dionemixt.with5-chloro-6-((2-iminopyrrolidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione(1:1)hydrochloride Request for quotationCAS: 733030-01-8
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