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1198221-21-4

1198221-21-4 structure
1198221-21-4 structure
  • Name: TAS-114
  • Chemical Name: TAS-114
  • CAS Number: 1198221-21-4
  • Molecular Formula: C21H29N3O6S
  • Molecular Weight: 451.54
  • Catalog: Research Areas Cancer
  • Create Date: 2019-06-01 16:25:21
  • Modify Date: 2025-08-25 14:19:03
  • TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1].

Name TAS-114
Description TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1].
Related Catalog
Target

dUTPase, DPD

In Vitro 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: HeLa, NUGC-4, NCI-H441, HT-29, CFPAC-1, and MCF-7 cell lines Concentration: 72 hours Incubation Time: 1 μM, 3 μM, and 10 μM Result: Clearly increased the cytotoxicity of FdUrd and 5-FU against various cancer cell lines in dose-dependent manner.
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.

Molecular Formula C21H29N3O6S
Molecular Weight 451.54
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