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TAS-114 

Cat. No.: HY-124062 Purity: 98.82%
Handling Instructions

TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.

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

TAS-114 Chemical Structure

TAS-114 Chemical Structure

CAS No. : 1198221-21-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1].

IC50 & Target

dUTPase, DPD

In Vitro

TAS-114 (1-10 μM; 72 hours) increases the cytotoxicity of 5-Fluorouracil (5-FU) and 5-FU,2′-deoxy-5-fluorouridine (FdUrd) against various cancer cell lines in dose-dependent manner[1].

Cell Cytotoxicity Assay[1]

Cell Line: HeLa, NUGC-4, NCI-H441, HT-29, CFPAC-1, and MCF-7 cell lines
Concentration: 72 hours
Incubation Time: 1 μM, 3 μM, and 10 μM
Result: Clearly increased the cytotoxicity of FdUrd and 5-FU against various cancer cell lines in dose-dependent manner.
In Vivo

TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice[1].

Animal Model: BALB/c nude mice with MX-1 human breast cancer xenografts[1]
Dosage: 37.5 to 1,200 mg/kg/day
Administration: Orally; daily; 1-14 days
Result: Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice.
Clinical Trial
Molecular Weight

451.54

Formula

C₂₁H₂₉N₃O₆S

CAS No.

1198221-21-4

SMILES

O=S(CCCOCN(C(N1)=O)C=CC1=O)(N[[email protected]@H](C2=CC=CC(OC3CCCC3)=C2)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2146 mL 11.0732 mL 22.1464 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 mL
10 mM 0.2215 mL 1.1073 mL 2.2146 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (11.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (11.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (11.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.82%

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Keywords:

TAS-114TAS114TAS 114OthersInhibitorinhibitorinhibit

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Product name:
TAS-114
Cat. No.:
HY-124062
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