Name: TAS-102 (Trifluridine/Tipiracil Hydrochloride Mixture)
Brand: Selleck Chemicals
SKU: S8539
Availability: InStock
Rating: 5 (5 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other Thymidylate Synthase Inhibitors	Raltitrexed

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (199.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 29 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL 87 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	435.76	Formula	C₁₀H₁₁F₃N₂O₅.0.5C₉H₁₁ClN₄O₂.0.5HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	733030-01-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Trifluridine-Tipiracil Hydrochloride Mixture			SMILES	Cl.OCC1OC(CC1O)N2C=C(C(=O)NC2=O)C(F)(F)F.OCC3OC(CC3O)N4C=C(C(=O)NC4=O)C(F)(F)F.ClC5=C(CN6CCCC6=N)NC(=O)NC5=O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

In vitro	TAS-102 is an oral combination drug consisting of trifluridine (FTD), which is a thymidine-based nucleoside analog, and tipiracil hydrochloride (TPI), which improves the bioavailability of FTD by inhibiting its catabolism by thymidine phosphorylase (TP). Phosphorylated form of trifluridine is incorporated into DNA resulting in DNA dysfunction and cell cycle arrest. Thymidine phosphorylase inhibitor inhibits degradation of FTD and inhibits angiogenesis. Thus, this compound treatment results in massive trifluridine incorporation into DNA and in activation of similar DNA damage response pathways, which involve phosphorylation of Chk1 and cycle arrest during the G2/M-phase.
In vivo	The elimination half-life of FTD after intravenous administration to humans is very rapid (18 minutes), due to the rapid degradation of FTD to its major metabolite, 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione. In monkeys, the plasma FTD level after oral administration alone is very low, suggesting extensive first-pass metabolism by the liver and intestine TPase. However, the addition of TPI(tipiracil hydrochloride) is found to enable oral administration. By inhibiting TP, TPI inhibits the degradation of FTD in the liver and intestines following oral administration and thereby improves its bioavailability. The TP enzyme catalyzes the phosphorolysis of pyrimidine 2'-deoxynucleosides such as FTD. Studies using human CRC tumor xenografts in mice determine that the maximum antitumor activity is achieved with a 1:0.5 molar ratio, and studies in mice and monkeys show that the maximum plasma concentration of FTD is almost achieved with the same ratio. Moreover, this ratio produces a favorable balance between antitumor activity and toxicity. Lower toxicity in mice is observed with TPI coadministration than with FTD alone. This compound can overcome acquired resistance to 5-FU because the main mechanism of this chemical is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. It has demonstrated efficacy in 5-FU-refractory cancers.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26428513/ [2] https://pubmed.ncbi.nlm.nih.gov/26254349/ [3] https://pubmed.ncbi.nlm.nih.gov/31154566/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-18)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07656038	NOT_YET_RECRUITING	Colonrectal Cancer (CRC)	STCube, Inc.	2026-06-30	PHASE1
NCT05854498	RECRUITING	Metastatic Colorectal Cancer	University of Wisconsin, Madison	2023-10-13	PHASE2
NCT07649655	NOT_YET_RECRUITING	Unresectable/Metastatic Colorectal Cancer	Shanghai EpimAb Biotherapeutics Co., Ltd.	2026-07	PHASE1
NCT06699836	ACTIVE_NOT_RECRUITING	Metastatic Colorectal Cancer (mCRC)	CytoDyn, Inc.	2025-06-16	PHASE2
NCT06992258	RECRUITING	Colorectal Cancer	Criterium, Inc.	2025-10-27	PHASE2
NCT07371871	NOT_YET_RECRUITING	Advanced Gastric Cancer	Anhui Provincial Cancer Hospital	2026-01-08

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TAS-102 (Trifluridine/Tipiracil Hydrochloride Mixture) Nucleoside Antitumour Agent

Chemical Structure

Molecular Weight: 435.76