Ethaselen|217798-39-5|(BBSKE)-陌孚医药/Medlife

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Ethaselen (Synonyms: BBSKE)

目录号: PL12476 纯度: ≥98.0%

CAS No. :217798-39-5

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中文名称	Ethaselen
英文名称	Ethaselen
英文别名	ethaselen;4Q2EZS1IWG;2-[2-(3-oxo-1,2-benzoselenazol-2-yl)ethyl]-1,2-benzoselenazol-3-one;(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane;US8592468, EbSe14;BDBM50385303;DB15051;2,2'-Ethylenebis[1,2-benzisoselenazole-3(2H)-one];2,2'-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2H)-one) .;Ethaselen
Cas No.	217798-39-5
分子式	C₁₆H₁₂N₂O₂Se₂
分子量	422.20
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Ethaselen (BBSKE) 是具有口服活性的，选择性的硫氧还蛋白还原酶 (TrxR) 抑制剂，对野生型人 TrxR1 和大鼠 TrxR1 的 IC₅₀ 分别为 0.5 和 0.35 μM。Ethaselen 特异性结合哺乳动物 TrxR1 C 端活性位点中独特的硒代半胱氨酸-半胱氨酸氧化还原对。Ethaselen 是一种有机硒化合物，一种有效的抗肿瘤候选药物，可通过靶向 TrxR 对非小细胞肺癌 (NSCLC) 发挥有效抑制作用。

生物活性

Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.

性状

Solid

IC50 & Target[1][2]

TrxR

体外研究(In Vitro)

Ethaselen (2.5-10 μM; 12, 24 hours) suppresses A549 cell viability in a both concentration- and time-dependent manner. H1666, which has considerably lower TrxR1 expression level, is less susceptible to 24 h treatment with Ethaselen.
Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively.
Ethaselen (2.5-10 μM; 12, 24 hours) has no effect on the protein amounts of TrxR1 and Trx. The mRNA level of TrxR1 does not show significant alteration in Ethaselen-treated A549 cells.
Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells.
Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells.
The inhibition constants for Ethaselen binding to free enzyme (K

体内研究(In Vivo)

Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Five

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Lihui Wang, et al. Ethaselen: a potent mammalian thioredoxin reductase 1 inhibitor and novel organoselenium anticancer agent. Free Radic Biol Med. 2012 Mar 1;52(5):898-908.
[2]. Suo-Fu Ye, et al. Dose-biomarker-response modeling of the anticancer effect of ethaselen in a human non-small cell lung cancer xenograft mouse model. Acta Pharmacol Sin. 2017 Feb;38(2):223-232.

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (29.61 mM; ultrasonic and warming and heat to 60°C)配制储备液

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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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