TAS-114|1198221-21-4|-陌孚医药/Medlife

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TAS-114

目录号: PL08488 纯度: ≥99%

TAS-114 是 dUTPase 和二氢嘧啶脱氢酶 (DPD) 的双靶点抑制剂，可提高氟嘧啶药物的疗效。

CAS No. :1198221-21-4

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中文名称	TAS-114
英文名称	TAS-114
英文别名	TAS-114;N-[(1R)-1-[3-(Cyclopentyloxy)-phenyl]-ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]-1-propanesulfonamide;BDBM101745;(R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide;US8530490, 5;FKM;N-[(1R)-1-(3-cyclopentyloxyphenyl)ethyl]-3-[(2,4-dioxopyrimidin-1-yl)methoxy]propane-1-sulfonamide
Cas No.	1198221-21-4
分子式	C₂₁H₂₉N₃O₆S
分子量	451.54
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

TAS-114 是 dUTPase 和二氢嘧啶脱氢酶 (DPD) 的双靶点抑制剂，可提高氟嘧啶药物的疗效。

生物活性

TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.

性状

Solid

IC50 & Target[1][2]

dUTPase, DPD

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (221.46 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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