Trifluridine/tipiracil hydrochloride mixture

Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha, alpha, alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI) . Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA[1][2].

Product Specifications

CAS Number

[733030-01-8]

Product Name Alternative

TAS-102; FTD/TPI

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Nucleoside Antimetabolite/Analog; Thymidylate Synthase

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TAS-102.html

Purity

99.98

Solubility

DMF : 20 mg/mL (ultrasonic) |DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C1N([C@H]2C[C@H](O)[C@@H](CO)O2)C=C(C(F)(F)F)C(N1)=O.O=C3NC(CN4CCCC4=N)=C(Cl)C(N3)=O.[1/2].Cl

Molecular Formula

C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl

Molecular Weight

435.76

Precautions

H302, H315, H319, H335

References & Citations

[1]Emura T, et al. A novel antimetabolite, TAS-102 retains its effect on FU-related resistant cancer cells. Int J Mol Med. 2004;13 (4) :545-549.|[2]Nukatsuka M, et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts. Anticancer Res. 2015;35 (3) :1437-1445.|[3]Limagne E, Thibaudin M, Nuttin L, et al. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019;7 (12) :1958-1969. |[4]Suzuki N, Nakagawa F, Takechi T. Trifluridine/tipiracil increases survival rates in peritoneal dissemination mouse models of human colorectal and gastric cancer [published correction appears in Oncol Lett. 2021 Jul;22 (1) :511]. Oncol Lett. 2017;14 (1) :639-646.