TAS-102
Modify Date: 2026-07-07 11:14:22
TAS-102 structure
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Common Name | TAS-102 | ||
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| CAS Number | 733030-01-8 | Molecular Weight | 435.76 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of TAS-102Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio. |
This table lists Chinese names, IUPAC names and various aliases of this chemical substance.
| Name | 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride |
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| Synonym | More Synonyms |
This table contains bioactivity, target information and biological‑assay experimental data of this compound.
| Description | Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio. |
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| Related Catalog | |
| In Vitro | Trifluridine-tipiracil hydrochloride mixture (TAS-102), a novel antimetabolite combination chemotherapy agent, consists of a rediscovered antimetabolite agent, trifluorothymidine (trifluridine, FTD) combined with the metabolic inhibitor of thymidine phosphorylase, tipiracil (TPI), in a 1:0.5 molar ratio[1]. FTD is the active antitumor component of Trifluridine-tipiracil hydrochloride mixture (TAS-102); its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells. The incorporation into DNA is known to have antitumor effects, since the inhibition of thymidylate synthase caused by oral FTD rapidly disappears after the drug's elimination. When FTD is administered orally, it is rapidly degraded to its inactive form by thymidine phosphorylase in the intestines and liver (first-pass effect). Consequently, TPI is synthesized to maintain adequate plasma concentrations of orally-administered FTD and to potentiate the antitumor activity of FTD[2]. |
| In Vivo | Trifluridine-tipiracil hydrochloride mixture (TAS-102) and CPT-11 is a promising treatment option for colorectal or gastric cancer. Trifluridine-tipiracil hydrochloride mixture monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. The combination-treated (CPT-11-and Trifluridine-tipiracil hydrochloride mixture) group is significantly superior to monotherapy[2]. FTD systemic exposure in plasma increaseS dose-dependently. The tumor growth rate and body weight gain decreaseS dose-dependently, but FTD concentrations in the DNA of tumor tissues and white blood cells increases dose-dependently. FTD inhibits colony formation of bone marrow cells in a concentration-dependent manner[3]. |
| Animal Admin | Mice: Trifluridine-tipiracil hydrochloride mixture is prepared by mixing FTD and TPI at a molar ratio of 1:0.5 in 0.5% HPMC. The dose of TAS-102 is expressed according to the amount of FTD. Trifluridine-tipiracil hydrochloride mixture is administered orally from day 1 to 14, twice a day, with approximately a 6-hour interval at the reported effective dose (150 mg/kg/day) (7,11). For the control group, 0.5% HPMC alone is administered at 10 ml/kg according to a similar schedule. CPT-11 (40 mg/kg) is administered intravenously on days 1 and 8, once a day. The tumor diameters are measured twice a week, and the tumor volume is estimated[2]. |
| References |
This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.
| Molecular Formula | C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl |
|---|---|
| Molecular Weight | 435.76 |
| PSA | 104.81000 |
| Storage condition | -20℃ |
This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.
| TAS 102 |
| Tipiracil hydrochloride mixture with Trifluridine |
| Tipiracil / Trifluridine |
| Tipiracil hydrochloride / Trifluridine |
| Viroptic mixture with 5-CIMU |
| TAS-102 |
This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.
| Q: What is the English name of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: The English name of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride is 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride. |
| Q: What is the molecular weight of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: Molecular weight of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride is 435.76. |
| Q: What English synonyms does 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride have? |
| A: English synonyms of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride: TAS 102, Tipiracil hydrochloride mixture with Trifluridine, Tipiracil / Trifluridine, Tipiracil hydrochloride / Trifluridine, Viroptic mixture with 5-CIMU, TAS-102. |
| Q: What is the polar surface area (PSA) of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: Polar surface area (PSA) of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride is 104.81000. |
| Q: What is the CAS number of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: CAS number of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride is 733030-01-8. |
| Q: What is the molecular formula of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: Molecular formula of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride is C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl. |
| Q: What are the storage conditions for 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: Storage conditions for 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride: -20℃. |
| Q: What are the uses of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride? |
| A: Main uses of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione,1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione,hydrochloride: Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio. |
This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.
| Shanghai Nianxing Industrial Co., Ltd |