| Description | 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 induces apoptosis in cancer cells and inhibits the proliferation of colorectal cancer cells. |
| In vitro | 在 A549 细胞中，Ethaselen（2.5、5、7.5、10 μM；12、24小时）以浓度和时间依赖的方式抑制了 A549 细胞的存活率[1]。 |
| In vivo | 在 A549 细胞中，以 5 周大的雌性 BALB/c 裸鼠作为实验模型，以 Ethaselen（36、72、108 mg/kg；PO；每日；连续10天）处理后，显示出对肿瘤生长的抑制增加，且抑制水平随剂量增加而增加[2]。 |
| Synonyms | BBSKE |
| molecular weight | 422.2 |
| Molecular formula | C16H12N2O2Se2 |
| CAS | 217798-39-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10 mg/mL (23.69 mM), Sonication is recommended. |
| 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. 3. Wu W, et al.A thioredoxin reductase inhibitor ethaselen induces growth inhibition and apoptosis in gastric cancer. J Cancer. 2020 Mar 4;11(10):3013-3019. |