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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Nucleoside Antimetabolite/Analog-TAS-114
TAS-114

Chemical Structure : TAS-114

CAS No.: 1198221-21-4

TAS-114 (TAS114)

货号: PC-63498Not For Human Use, Lab Use Only.

TAS-114 is a first-in-class, potent, dual dUTPase/DPD (dihydropyrimidine dehydrogenase) inhibitor with Ki of 0.13/2.14 uM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAS-114 is a first-in-class, potent, dual dUTPase/DPD (dihydropyrimidine dehydrogenase) inhibitor with Ki of 0.13/2.14 uM, respectively.
TAS-114 competitively inhibits dUTPase in the dUTP binding step, selectively inhibits the hydrolysis of dUTP to dUMP in cancer cells, significantly enhances cytotoxicity of fluoropyrimidines.
TAS-114 has moderate and reversible inhibitory activity on dihydropyrimidine dehydrogenase (DPD), a catabolizing enzyme of 5-FU; increases the bioavailability of 5-FU when co-administered with capecitabine in mice, significantly improves the therapeutic efficacy of capecitabine in vivo.

物理化学性质&存储条件

分子量 451.538
分子式 C21H29N3O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(1R)-1-[3-(cyclopentyloxy)phenyl]-ethyl]-3-[(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy]-1-propanesulfonamide

参考文献

1. Yano W, et al. Mol Cancer Ther. 2018 May 10. pii: molcanther.0911.2017.

2. Saito K, et al. Cancer Chemother Pharmacol. 2014 Mar;73(3):577-83.

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