1. Cell Cycle/DNA Damage
    Apoptosis
  2. Nucleoside Antimetabolite/Analog
    Thymidylate Synthase
  3. Trifluridine-tipiracil hydrochloride mixture

Trifluridine-tipiracil hydrochloride mixture (Synonyms: TAS-102)

Cat. No.: HY-16478 Purity: 99.72%
Handling Instructions

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.

For research use only. We do not sell to patients.

Trifluridine-tipiracil hydrochloride mixture Chemical Structure

Trifluridine-tipiracil hydrochloride mixture Chemical Structure

CAS No. : 733030-01-8

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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.

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2.34 mg/mL (5.37 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2948 mL 11.4742 mL 22.9484 mL
5 mM 0.4590 mL 2.2948 mL 4.5897 mL
10 mM 0.2295 mL 1.1474 mL 2.2948 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

435.76

Formula

C₁₀H₁₁F₃N₂O₅ . ₁/₂C₉H₁₁ClN₄O₂ . ₁/₂HCl

CAS No.

733030-01-8

SMILES

O=C1N([[email protected]]2C[[email protected]](O)[[email protected]@H](CO)O2)C=C(C(F)(F)F)C(N1)=O.O=C3N([[email protected]]4C[[email protected]](O)[[email protected]@H](CO)O4)C=C(C(F)(F)F)C(N3)=O.O=C5NC(CN6CCCC6=N)=C(Cl)C(N5)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Trifluridine-tipiracil hydrochloride mixture
Cat. No.:
HY-16478
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Trifluridine-tipiracil hydrochloride mixture

Cat. No.: HY-16478