Chemical Structure : TAS-114
CAS No.:
1198221-21-4
TAS-114
(TAS114)
Catalog No.: PC-63498Not For Human Use, Lab Use Only.
TAS-114 is a first-in-class, potent, dual dUTPase/DPD inhibitor with Ki of 0.13/2.14 uM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TAS-114 is a first-in-class, potent, dual dUTPase/DPD inhibitor with Ki of 0.13/2.14 uM, respectively; competitively inhibits dUTPase in the dUTP binding step, selectively inhibits the hydrolysis of dUTP to dUMP in cancer cells, significantly enhances cytotoxicity of fluoropyrimidines; TAS-114 has moderate and reversible inhibitory activity on dihydropyrimidine dehydrogenase (DPD), a catabolizing enzyme of 5-FU; increases the bioavailability of 5-FU when co-administered with capecitabine in mice, significantly improves the therapeutic efficacy of capecitabine in vivo.
Gastric Cancer
Phase 2 Clinical
Physicochemical Properties
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M.Wt
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451.538
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Formula
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C21H29N3O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-[(1R)-1-[3-(cyclopentyloxy)phenyl]-ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]-1-propanesulfonamide
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References
1. Yano W, et al. Mol Cancer Ther. 2018 May 10. pii: molcanther.0911.2017.
2. Saito K, et al. Cancer Chemother Pharmacol. 2014 Mar;73(3):577-83.
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