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. Price and Availability

TAS-114 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually 98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.1198221-21-4 (R-isomer)Synonym: TAS-114, TAS 114, TAS114IUPAC/Chemical Name: (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamideInChi Key: AMCGLRWKUQPNKD-MRXNPFEDSA-NInChi 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/s1SMILES Code: O=C1NC(N(COCCCS(=O)(N[C@H](C)C2=CC=CC(OC3CCCC3)=C2)=O)C=C1)=O Technical Data 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. Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

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.

References

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.

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