Ethaselen

• CAT Number: I006726
• CAS Number: 217798-39-5
• Molecular Formula: C16H12N2O2Se2
• Molecular Weight: 422.2
• Purity: ≥95%
• Synonyms: Ethaselen; 1 2bis (12benzisoselenazolone3 (2H)ketone) ethane BBSKE.;2,2/’-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2H)-one) .
• Target: thioredoxin reductase inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term

Ethaselen, also known as BBSKE, is a novel organoselenium thioredoxin reductase inhibitor, is currently being investigated in a phase I clinical trial in China. Ethaselen enhanced the efficacy of radiation therapy both in vivo and in vitro without observable toxicity. BBSKE was found to suppress irradiation-induced NF-κB activation dramatically when using A549 cells stably transfected with NF-κB luciferase reporter. Ethaselen is a potentially promising agent for the treatment of patients with NSCLC clinically.

Reference

1:Ethaselen: a novel organoselenium anticancer agent targeting thioredoxin reductase 1 reverses cisplatin resistance in drug-resistant K562 cells by inducing apoptosis. Ye SF, Yang Y, Wu L, Ma WW, Zeng HH.J Zhejiang Univ Sci B. 2017 May;18(5):373-382. doi: 10.1631/jzus.B1600073. PMID: 28471109 2:Dose-biomarker-response modeling of the anticancer effect of ethaselen in a human non-small cell lung cancer xenograft mouse model. Ye SF, Li J, Ji SM, Zeng HH, Lu W.Acta Pharmacol Sin. 2017 Feb;38(2):223-232. doi: 10.1038/aps.2016.114. Epub 2016 Dec 5. PMID: 27917873 Free PMC Article3:Synergistic inhibition of sunitinib and ethaselen against human colorectal cancer cells proliferation. Zheng X, Zhang Y, Zhang L, Xu W, Ma W, Sun R, Zeng H.Biomed Pharmacother. 2016 Oct;83:212-220. doi: 10.1016/j.biopha.2016.06.040. Epub 2016 Jun 30. PMID: 27372405 4:Synergistic effect of ethaselen and selenite treatment against A549 human non-small cell lung cancer cells. Xu W, Ma WW, Zeng HH.Asian Pac J Cancer Prev. 2014;15(17):7129-35. PMID: 25227802 Free Article5:Ethaselen: a potent mammalian thioredoxin reductase 1 inhibitor and novel organoselenium anticancer agent. Wang L, Yang Z, Fu J, Yin H, Xiong K, Tan Q, Jin H, Li J, Wang T, Tang W, Yin J, Cai G, Liu M, Kehr S, Becker K, Zeng H.Free Radic Biol Med. 2012 Mar 1;52(5):898-908. doi: 10.1016/j.freeradbiomed.2011.11.034. Epub 2011 Dec 21. PMID: 22210352 6:Selenium-containing thioredoxin reductase inhibitor ethaselen sensitizes non-small cell lung cancer to radiotherapy. Wang L, Fu JN, Wang JY, Jin CJ, Ren XY, Tan Q, Li J, Yin HW, Xiong K, Wang TY, Liu XM, Zeng HH.Anticancer Drugs. 2011 Sep;22(8):732-40. doi: 10.1097/CAD.0b013e32834618bc. PMID: 21562407 7:Novel mechanism of ethaselen in poorly differentiated colorectal RKO cell growth inhibition: Simultaneous regulation of TrxR transcription, expression and enzyme activity. Yin H, Li J, Xiong K, Wang L, Wang T, Tan Q, Fu J, Ren X, Zeng H.Differentiation. 2011 Jan;81(1):49-56. doi: 10.1016/j.diff.2010.09.180. PMID: 20864247 8:Thioredoxin reductase inhibitor ethaselen increases the drug sensitivity of the colon cancer cell line LoVo towards cisplatin via regulation of G1 phase and reversal of G2/M phase arrest. Fu JN, Li J, Tan Q, Yin HW, Xiong K, Wang TY, Ren XY, Zeng HH.Invest New Drugs. 2011 Aug;29(4):627-36. doi: 10.1007/s10637-010-9401-y. Epub 2010 Mar 2. PMID: 20195699 9:Augmented antitumor effects of combination therapy of cisplatin with ethaselen as a novel thioredoxin reductase inhibitor on human A549 cell in vivo. Tan Q, Li J, Yin HW, Wang LH, Tang WC, Zhao F, Liu XM, Zeng HH.Invest New Drugs. 2010 Jun;28(3):205-15. doi: 10.1007/s10637-009-9235-7. Epub 2009 Mar 7. PMID: 19271154 10:Self-assembled polymeric micellar nanoparticles as nanocarriers for poorly soluble anticancer drug ethaselen. Li X, Yang Z, Yang K, Zhou Y, Chen X, Zhang Y, Wang F, Liu Y, Ren L.Nanoscale Res Lett. 2009 Sep 16;4(12):1502-11. doi: 10.1007/s11671-009-9427-2. PMID: 20652138 Free PMC Article