The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. 103-76-4, formula is C6H14N2O, Name is N-(2-Hydroxyethyl)piperazine. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Electric Literature of 103-76-4.
Liu, Haixia;Ding, Xinyu;Liu, Linyi;Mi, Qianglong;Zhao, Quanju;Shao, YuBao;Ren, Chaowei;Chen, Jinju;Kong, Ying;Qiu, Xing;Elvassore, Nicola;Yang, Xiaobao;Yin, Qianqian;Jiang, Biao research published 《 Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation》, the research content is summarized as follows. Protein degradation is a promising strategy for drug development. Proteolysis-targeting chimeras (PROTACs) hijacking the E3 ligase cereblon (CRBN) exhibit enormous potential and universal degradation performance due to the small mol. weight of CRBN ligands. In this study, the CRBN-recruiting PROTACs were explored on the degradation of oncogenic fusion protein BCR-ABL, which drives the pathogenesis of chronic myeloid leukemia (CML). A series of novel PROTACs were synthesized by conjugating BCR-ABL inhibitor dasatinib to the CRBN ligand including pomalidomide and lenalidomide, and the extensive structure-activity relationship (SAR) studies were performed focusing on optimization of linker parameters. Therein, we uncovered that pomalidomide-based degrader 17 (SIAIS056), possessing sulfur-substituted carbon chain linker, exhibits the most potent degradative activity in vitro and favorable pharmacokinetics in vivo. Besides, degrader 17 also degrades a variety of clin. relevant resistance-conferring mutations of BCR-ABL. Furthermore, degrader 17 induces significant tumor regression against K562 xenograft tumors. Our study indicates that 17 as an efficacious BCR-ABL degrader warrants intensive investigation for the future treatment of BCR-ABL+ leukemia.
103-76-4, 1-(2-Hydroxyethyl)piperazine is a useful research compound. Its molecular formula is C6H14N2O and its molecular weight is 130.19 g/mol. The purity is usually 95%.
1-(2-Hydroxyethyl)piperazine is a chemical solvent that is used for the absorption of amines and other compounds. It has been shown to have a high affinity for acidic substances, which may be due to its ability to form hydrogen bonds with them. 1-(2-Hydroxyethyl)piperazine is also used in sample preparation for the analysis of amines and other compounds in fruit extracts. The solubility of 1-(2-Hydroxyethyl)piperazine depends on the experimental conditions, including pH, temperature, and pressure. FT-IR spectroscopy has been used to measure the vibrational modes of 1-(2-Hydroxyethyl)piperazine molecules. The IR spectrum revealed that this compound contains a hydroxyl group and two fatty acid chains with one or more hydroxyl groups at their terminal end. The nmr spectrum showed that 1-(2-Hydroxyethyl)piperazine contains an NH proton as well as, Electric Literature of 103-76-4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics