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TAS-102 is an orally administered combination of trifluridine and Tipiracil hydrochloride in a molar ratio of 1:0.5. Trifluridine is the active antitumor component of TAS-102; its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells.
In vivo, TAS-102 monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. TAS-102 can overcome acquired resistance to 5-FU because the main mechanism of TAS-102 is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has demonstrated efficacy in 5-FU-refractory cancers.
| Molecular Weight | 575.32 |
| Formula | C19H23Cl2F3N6O7 |
| CAS Number | 733030-01-8 |
| Solubility (25°C) | Water 50 mg/mL Ethanol 20 mg/mL DMSO 10 mg/mL (ultrasonic and warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Uboha N, et al. Future Oncol. TAS-102: a novel antimetabolite for the 21st century.
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