TAS-114

Research use only, not for human use.

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

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.

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Animal Model:BALB/c nude mice with MX-1 human breast cancer xenograftsDosage:37.5 to 1,200 mg/kg/day Administration:Orally; daily; 1-14 days Result:Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice.

TAS114

Cell Cycle/DNA Damage

Nucleoside Antimetabolite/Analog

Nucleoside Antimetabolite/Analog

Cancer

Gastric Cancer

1198221-21-4

451.538

C21H29N3O6S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (221.46 mM)

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

N-[(1R)-1-[3-(cyclopentyloxy)phenyl]-ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]-1-propanesulfonamide

(-20℃)

With Ice Pack

≥ 2 years