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Ethaselen (BBSKE) is a novel, oral and potent organoselenium-based inhibitor of thioredoxin reductase (TrxR) with potential anticancer activity. It inhibits wild-type human TrxR1 and rat TrxR1 with IC50 values of 0.5 and 0.35 μM, respectively. Ethaselen is under investigation in clinical trials in China for cancer (NSCLC) treatment.
| ln Vitro |
A549 cell viability is inhibited by ethaselen (2.5-10 μM; 12-24 hours) in a concentration- and time-dependent manner. H1666 responds less well to a 24-hour Ethaselen therapy and has a relatively low TrxR1 expression level [1]. The activity of TrxR1 in cells is inhibited by the inhibition approach; the IC50 values after 12 and 24 hours of treatment are 4.2 and 2 μM, respectively [1]. Ethaselen (2.5–10 μM; 12–24 hours) has no effect on TrxR1 and Trx protein levels. TrxR1 mRNA level in A549 cells treated with ethaselen did not change significantly [1]. In A549 cells, ethaselen (2.5–50 μM; 1–24 hours) induces intracellular Trx oxidation [1]. 12, 24 hours) significantly increased the amount of ROS in A549 cells in a concentration-dependent manner [1]. The enzyme's free and substrate complex inhibitory concentrations (Kis) for ethaselen are 0.022 and 0.087 μM, respectively. Moreover, etaselen has the ability to create a time-dependent covalent Se-S bond with Trx's Cys497 to prevent TrxR1 from being occupied [1].
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| ln Vivo |
In a dose-dependent manner, ethaselen (BBSKE; 36-108 mg/kg/day; sidewall for 10 days) promotes the suppression of tumor growth [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 cell Tested Concentrations: 2.5, 5, 7.5, 10 μM Incubation Duration: 12, 24 hrs (hours) Experimental Results: Inhibits A549 cell viability in a concentration- and time-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 5weeks old female BALB/c nude mice A549 cells [2]
Doses: 36, 72, 108 mg/kg Route of Administration: oral; daily; 10 days Experimental Results: demonstrated enhanced inhibitory effect on tumor growth , and the level of inhibition increases with increasing dose. The TrxR activity level in the high-dose group (108 mg/kg) diminished more than that in the mid-dose group (72 mg/kg) and low-dose group (36 mg/kg). |
| 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.
[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. |
| Molecular Formula |
C16H12N2O2SE2
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|---|---|
| Molecular Weight |
422.2
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| Exact Mass |
423.92292
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| CAS # |
217798-39-5
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| SMILES |
O=C1N(CCN2[Se]C3=CC=CC=C3C2=O)[Se]C4=CC=CC=C14
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| InChi Key |
SFFSGPCYJCMDJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12N2O2Se2/c19-15-11-5-1-3-7-13(11)21-17(15)9-10-18-16(20)12-6-2-4-8-14(12)22-18/h1-8H,9-10H2
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| Chemical Name |
2,2'-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2H)-one) .
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| Synonyms |
BBSKE EB Ethaselen
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~29.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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