TAS-114

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206624

CAS#: 1198221-21-4 (R-isomer)

Description: TAS-114 is a first-in-class oral deoxyuridine triphosphatase (dUTPase) inhibitor, which acts as a modulator of the pyrimidine nucleotide metabolic pathway. dUTPase may protect cancer cells from aberrant base mediated cytotoxicity during thymidylate synthase (TS) inhibition, and its overexpression is associated with resistance to TS inhibitors.


Chemical Structure

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TAS-114
CAS# 1198221-21-4 (R-isomer)

Theoretical Analysis

MedKoo Cat#: 206624
Name: TAS-114
CAS#: 1198221-21-4 (R-isomer)
Chemical Formula:
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis:

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1198221-48-5 (Racemic)   1198221-21-4 (R-isomer),  

Synonym: TAS-114, TAS 114, TAS114

IUPAC/Chemical Name: (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide

InChi Key: AMCGLRWKUQPNKD-MRXNPFEDSA-N

InChi Code: InChI=1S/C21H29N3O6S/c1-16(17-6-4-9-19(14-17)30-18-7-2-3-8-18)23-31(27,28)13-5-12-29-15-24-11-10-20(25)22-21(24)26/h4,6,9-11,14,16,18,23H,2-3,5,7-8,12-13,15H2,1H3,(H,22,25,26)/t16-/m1/s1

SMILES Code: O=C1NC(N(COCCCS(=O)(N[C@H](C)C2=CC=CC(OC3CCCC3)=C2)=O)C=C1)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Note: Many vendors listed a wrong chemical structure of TAS-114. The new chemical structure just published in below paper: TAS-​114, a First-​in-​Class Dual dUTPase​/DPD Inhibitor, Demonstrates Potential to Improve Therapeutic Efficacy of Fluoropyrimidine-​Based Chemotherapy By Yano, Wakako; Yokogawa, Tatsushi; Wakasa, Takeshi; Yamamura, Keisuke; Fujioka, Akio; Yoshisue, Kunihiro; Matsushima, Eiji; Miyahara, Seiji; Miyakoshi, Hitoshi; Taguchi, Junko; et al From Molecular Cancer Therapeutics (2018), 17(8), 1683-1693.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 0.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Doi T, Yoh K, Shitara K, Takahashi H, Ueno M, Kobayashi S, Morimoto M, Okusaka
T, Ueno H, Morizane C, Okano N, Nagashima F, Furuse J. First-in-human phase 1
study of novel dUTPase inhibitor TAS-114 in combination with S-1 in Japanese
patients with advanced solid tumors. Invest New Drugs. 2018 Dec 4. doi:
10.1007/s10637-018-0697-3. [Epub ahead of print] PubMed PMID: 30511200.


2: Yano W, Yokogawa T, Wakasa T, Yamamura K, Fujioka A, Yoshisue K, Matsushima E,
Miyahara S, Miyakoshi H, Taguchi J, Chong KT, Takao Y, Fukuoka M, Matsuo K.
TAS-114, a First-in-Class Dual dUTPase/DPD Inhibitor, Demonstrates Potential to
Improve Therapeutic Efficacy of Fluoropyrimidine-Based Chemotherapy. Mol Cancer
Ther. 2018 Aug;17(8):1683-1693. doi: 10.1158/1535-7163.MCT-17-0911. Epub 2018 May
10. PubMed PMID: 29748212.


3: Peters GJ. Novel developments in the use of antimetabolites. Nucleosides
Nucleotides Nucleic Acids. 2014;33(4-6):358-74. doi:
10.1080/15257770.2014.894197. Review. PubMed PMID: 24940694.


4: Saito K, Nagashima H, Noguchi K, Yoshisue K, Yokogawa T, Matsushima E, Tahara
T, Takagi S. First-in-human, phase I dose-escalation study of single and multiple
doses of a first-in-class enhancer of fluoropyrimidines, a dUTPase inhibitor
(TAS-114) in healthy male volunteers. Cancer Chemother Pharmacol. 2014
Mar;73(3):577-83. doi: 10.1007/s00280-014-2383-2. Epub 2014 Jan 23. PubMed PMID:
24452393.


5: Utsugi T. New challenges and inspired answers for anticancer drug discovery
and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53. doi:
10.1093/jjco/hyt131. Epub 2013 Sep 5. PubMed PMID: 24014883; PubMed Central
PMCID: PMC3787805.