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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
TAS-102 (a mixture of Trifluridine and tipiracil hydrochloride in a 1:0.5 molar ratio) is a combination drug under investigation for treating metastatic colorectal cancer. It is an oral bioavailable combination medication containing a powerful thymidine phosphorylase inhibitor called tiracil hydrochloride (TTP) and antineoplastic thymidine-based nucleoside analog called trifluridine (TFT) in a molar ratio of 1: 0.5.
| ln Vitro |
Trifluridine (FTD), a thymidine-based nucleoside analog, and tipiracil hydrochloride (TPI), an oral combination medication that increases the bioavailability of FTD by preventing thymidine phosphorylase (TP) from catabolizing it, make up TAS-102[1].
Trifluridine that has been phosphorylated is incorporated into DNA, causing DNA dysfunction and cell cycle arrest. Angiogenesis is inhibited and FTD degradation is inhibited by thymidine phosphorylase inhibitor. As a result, massive trifluridine incorporation into DNA and the activation of related DNA damage response pathways—which include cycle arrest during the G2/M-phase and Chk1 phosphorylation—are the outcomes of TAS-102 treatment[2]. |
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| ln Vivo |
Due to the fast breakdown of FTD into its main metabolite, 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione, the elimination half-life of FTD in humans following intravenous administration is extremely short (18 minutes). After oral administration alone, the plasma FTD level in monkeys is remarkably low, indicating extensive first-pass metabolism by the intestine and liver TPase. Oral administration is found to be made possible by the addition of TPI (tipiracil hydrochloride). By blocking TP, TPI increases the bioavailability of FTD by preventing its breakdown in the intestines and liver after oral administration. TP is an enzyme that catalyzes the phosphorolysis of FTD and other pyrimidine 2'-deoxynucleosides. The greatest antitumor activity is attained with a 1:0.5 molar ratio, according to studies conducted on human CRC tumor xenografts in mice. Similarly, studies conducted on mice and monkeys demonstrate that the maximum plasma concentration of FTD is nearly attained with the same ratio. Additionally, a good balance between toxicity and antitumor activity is produced by this ratio. When TPI is administered in addition to FTD, mice exhibit less toxicity. Because the primary mechanism of TAS-102 is unrelated to the primary metabolic enzymes of 5-FU, such as TS and OPRT, it can overcome acquired resistance to 5-FU. TAS-102 has proven effective in cancers that are resistant to 5-FU[1].
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| Cell Assay |
TAS-120 was applied to the cells in varying concentrations.
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| Animal Protocol |
Male nude mice bearing KM12C, KM12C/5-FU, DLD-1, DLD-1/5-FU, and SC-2 cells
150 mg/kg/day p.o.; twice a day for 14 days |
| References |
| Molecular Formula |
C19H23CL2F3N6O7
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|---|---|
| Molecular Weight |
575.3231
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| Elemental Analysis |
C, 39.67; H, 4.03; Cl, 12.32; F, 9.91; N, 14.61; O, 19.47
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| CAS # |
733030-01-8
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| Related CAS # |
70-00-8 (Trifluridie); 733030-01-8 (183204-72-0 (Tipiracil HCl)
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| Appearance |
Solid powder
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| SMILES |
O=C1NC(C(C(F)(F)F)=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2)=O.O=C3NC(C(Cl)=C(CN4C(CCC4)=N)N3)=O.[H]Cl
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| InChi Key |
PLIXOHWIPDGJEI-OJSHLMAWSA-N
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| InChi Code |
InChI=1S/C10H11F3N2O5.C9H11ClN4O2.ClH/c11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7;10-7-5(12-9(16)13-8(7)15)4-14-3-1-2-6(14)11;/h2,5-7,16-17H,1,3H2,(H,14,18,19);11H,1-4H2,(H2,12,13,15,16);1H/t5-,6+,7+;;/m0../s1
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| Chemical Name |
4-hydroxy-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-(trifluoromethyl)pyrimidin-2(1H)-one compound with 5-chloro-6-((2-iminopyrrolidin-1-yl)methyl)pyrimidine-2,4-diol (1:1) hydrochloride
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| Synonyms |
TAS-102; TAS102; TAS 102; Trifluridine/tipiracil hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~100 mg/mL (~229.5 mM)
DMF: ~20 mg/mL (~45.9 mM) DMSO: 2.3~87 mg/mL (5.4~199.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (114.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: 100 mg/mL (229.48 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7382 mL | 8.6908 mL | 17.3816 mL | |
| 5 mM | 0.3476 mL | 1.7382 mL | 3.4763 mL | |
| 10 mM | 0.1738 mL | 0.8691 mL | 1.7382 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04868773 | Active Recruiting |
Drug: Cabozantinib Drug: TAS-102 |
CRC Metastatic Cancer |
University of California, Irvine |
July 16, 2021 | Phase 1 |
| NCT04683965 | Active Recruiting |
Drug: TAS-102 Drug: Pemetrexed |
Colorectal Neoplasms | The First Affiliated Hospital with Nanjing Medical University |
January 1, 2021 | Phase 2 |
| NCT05600309 | Active Recruiting |
Drug: TAS-102 Drug: regorafenib |
Colorectal Cancer | Merck Sharp & Dohme LLC | June 14, 2022 | Phase 3 |
| NCT05064059 | Active Recruiting |
Drug: regorafenib Drug: TAS-102 |
Colorectal Cancer | Merck Sharp & Dohme LLC | November 10, 2021 | Phase 3 |
| NCT04776148 | Active Recruiting |
Drug: TAS-102 (trifluridine and tipiracil) Drug: regorafenib |
Colorectal Neoplasms | Merck Sharp & Dohme LLC | March 29, 2021 | Phase 3 |
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