WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206624
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.
Hodoodo Cat#: H206624
Name: TAS-114
CAS#: 1198221-21-4 (R-isomer)
Chemical Formula:
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis:
This product is not in stock, which may be available by custom synthesis.
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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: |
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.
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: |
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.