| Identification | Back Directory | [Name]
1-Propanesulfonamide, N-[(1R)-1-[3-(cyclopentyloxy)phenyl]ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]- | [CAS]
1198221-21-4 | [Synonyms]
TAS-114
TAS 114,TAS114
1-Propanesulfonamide, N-[(1R)-1-[3-(cyclopentyloxy)phenyl]ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]- | [Molecular Formula]
C21H29N3O6S | [MOL File]
1198221-21-4.mol | [Molecular Weight]
451.54 |
| Chemical Properties | Back Directory | [density ]
1.290±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, stored under nitrogen | [solubility ]
DMSO : 100 mg/mL (221.46 mM; Need ultrasonic) | [form ]
Solid | [pka]
9.36±0.10(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1]. | [in vivo]
TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice[1].
| Animal Model: | BALB/c nude mice with MX-1 human breast cancer xenografts[1] | | Dosage: | 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. |
| [References]
[1] Yano W, et al. 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 |
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