| Bioactivity | TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1]. |
| Target | dUTPase, DPD |
| Invitro | TAS-114 (1-10 μM; 72 hours) increases the cytotoxicity of 5-Fluorouracil (5-FU) and 5-FU,2′-deoxy-5-fluorouridine (FdUrd) against various cancer cell lines in dose-dependent manner[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| 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: |
| Name | TAS-114 |
| CAS | 1198221-21-4 |
| Formula | C21H29N3O6S |
| Molar Mass | 451.54 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [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. |