Ethaselen BBSKE|cas:217798-39-5|西域试剂

Ethaselen BBSKE,98.0%

产品编号：Bellancom-116749| CAS NO：217798-39-5| 分子式：C₁₆H₁₂N₂O₂Se₂| 分子量：422.20

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-116749	￥3000.00	杭州北京（现货）
Bellancom-116749	￥4900.00	杭州北京（现货）
Bellancom-116749	￥9800.00	杭州北京（现货）
Bellancom-116749	￥15000.00	杭州北京（现货）

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Ethaselen BBSKE

产品介绍

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活性分子，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 IC₅₀s 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.

体外研究

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_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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Five-week-old female BALB/c nude mice with A549 cell
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).

体内研究

Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Five-week-old female BALB/c nude mice with A549 cell
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).

体内研究

Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Five-week-old female BALB/c nude mice with A549 cell
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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (29.61 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3685 mL	11.8427 mL	23.6855 mL
5 mM	0.4737 mL	2.3685 mL	4.7371 mL
10 mM	0.2369 mL	1.1843 mL	2.3685 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.96 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.96 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。