TAS-114 | dUTPase/DPD inhibitor | Probechem Biochemicals

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 (dihydropyrimidine dehydrogenase) inhibitor with Ki of 0.13/2.14 uM, respectively.

Packing	Price	Stock
5 mg	$178	In stock
10 mg	$288	In stock
25 mg	$498	In stock
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Biological Activity

TAS-114 is a first-in-class, potent, dual dUTPase/DPD (dihydropyrimidine dehydrogenase) inhibitor with Ki of 0.13/2.14 uM, respectively.

TAS-114 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.

Physicochemical Properties

M.Wt	451.538
Formula	C21H29N3O6S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[(1R)-1-[3-(cyclopentyloxy)phenyl]-ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]-1-propanesulfonamide

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.

TAS-114 (TAS114)

Biological Activity

Physicochemical Properties

References

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