TAS-114 (C09-1182-884)

TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidineIn VitroTAS-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell 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 VivoTAS-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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice with MX-1 human breast cancer xenografts 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.Form:SolidIC50& Target:dUTPase, DPD. Specifications and Purity: 99%. Molecular Formula: C21H29N3O6S. Molecular Weight: 451.54. PubChem CID: 53630253. Isomeric SMILES: C[C@H](C1=CC(=CC=C1)OC2CCCC2)NS(=O)(=O)CCCOCN3C=CC(=O)NC3=O.