Ethaselen

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

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).

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Others

Other Targets

Others

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217798-39-5

422.2

C16H12N2O2Se2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 12.5 mg/mL (29.61 mM; 超声助溶 (<60°C)

O=C1C=2C=CC=CC2[Se]N1CCN3[Se]C=4C=CC=CC4C3=O

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(-20℃)

With Ice Pack

≥ 2 years