Ethaselen

Research use only, not for human use.

Ethaselen (BBSKE) is an orally active and selective thioredoxin reductase 1 (TrxR) inhibitor with anticancer activity that directly inhibits TrxR1 activity and is commonly used in combination with oxaliplatin to inhibit tumor growth.

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 : 12.5 mg/mL (29.61 mM; Ultrasonic (<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