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Ethaselen

产品编号 T39664 CAS 217798-39-5

别名: BBSKE

Ethaselen (BBSKE), a selective thioredoxin reductase (TrxR) inhibitor, is orally active with IC50s of 0.5 and 0.35 μM for wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair located in the C-terminal active site of mammalian TrxR1. As an organoselenium compound, it demonstrates potent antitumor activity against non-small cell lung cancer (NSCLC) by targeting TrxR.

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Ethaselen, CAS 217798-39-5

规格	价格/CNY	货期
2 mg	￥ 1,600	现货
5 mg	￥ 2,710	现货
25 mg	￥ 9,540	现货
50 mg	￥ 12,400	现货
1 mL * 10 mM (in DMSO)	￥ 3,250	现货

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生物活性

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存储 & 溶解度

参考文献

产品描述	Ethaselen (BBSKE), a selective thioredoxin reductase (TrxR) inhibitor, is orally active with IC50s of 0.5 and 0.35 μM for wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair located in the C-terminal active site of mammalian TrxR1. As an organoselenium compound, it demonstrates potent antitumor activity against non-small cell lung cancer (NSCLC) by targeting TrxR.
体外活性	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[1]. Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC 50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively[1]. 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[1]. Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells[1]. Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells[1]. The inhibition constants for Ethaselen binding to free enzyme (K i ) and the enzyme-substrate complex (K is ) were determined to be 0.022 and 0.087 μM, respectively. Ethaselen also inhibits mammalian TrxR1 in a time-dependent manner possibly by forming a covalent Se-S bond with Cys497 of Trx[1]. Cell Viability Assay[1]Cell Line: A549 cell Concentration: 2.5, 5, 7.5, 10 μM Incubation Time: 12, 24 hours Result: Suppressed A549 cell viability in a both concentration- and time-dependent manner.
体内活性	Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner[2]. Animal Model: Five-week-old female BALB/c nude mice with A549 cell[2]Dosage: 36, 72, 108 mg/kg Administration: PO; daily; for 10 days Result: Showed increased inhibition of tumor growth, and the inhibition levels increased with the dose. The TrxR activity levels of the high dose group (108 mg/kg) decreased more than the middle dose group (72 mg/kg) and low dose group (36 mg/kg).

别名	BBSKE
分子量	422.226
分子式	C16H12N2O2Se2
CAS No.	217798-39-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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