| Identification | Back Directory | [Name]
Ethaselen | [CAS]
217798-39-5 | [Synonyms]
BBSKE
Ethaselen
1,2-Benzisoselenazol-3(2H)-one, 2,2'-(1,2-ethanediyl)bis- | [Molecular Formula]
C16H12N2O2Se2 | [MOL File]
217798-39-5.mol | [Molecular Weight]
422.2 |
| Chemical Properties | Back Directory | [Boiling point ]
580.5±60.0 °C(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 12.5 mg/mL (29.61 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
-1.86±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
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).
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| [References]
[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. DOI:10.1016/j.freeradbiomed.2011.11.034
[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. DOI:10.1038/aps.2016.114 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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