Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N. It is structurally related to benzene, with one methine group (=CH−) replaced by a nitrogen atom. 766-11-0, formula is C5H3BrFN, Name is 5-Bromo-2-fluoropyridine. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Reference of 766-11-0.
Zhou, Bin;Liang, Xiaofei;Mei, Husheng;Qi, Shuang;Jiang, Zongru;Wang, Aoli;Zou, Fengming;Liu, Qingwang;Liu, Juan;Wang, Wenliang;Hu, Chen;Chen, Yongfei;Wang, Zuowei;Wang, Beilei;Wang, Li;Liu, Jing;Liu, Qingsong research published 《 Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas》, the research content is summarized as follows. The enhancer of zeste homolog 2 (EZH2) is the catalytic subunit of polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). Overexpression or mutation of EZH2 has been identified in hematol. malignancies and solid tumors. Based on the structure of EPZ6438 (1) and the binding model with PRC2, we designed a series of analogs aiming to improve the activities of EZH2 mutants. Structure-activity relationship (SAR) exploration at both enzymic and cellular levels led to the discovery of inhibitor 29. In the biochem. assay, 29 inhibited EZH2 (IC50 = 26.1 nM) with high selectivity over other histone methyltransferases. It was also potent against EZH2 mutants (EZH2 Y641F, IC50 = 72.3 nM). Furthermore, it showed no apparent inhibitory activity against the human ether-á-go-go related gene (hERG) (IC50 > 30μM). In vivo, 29 exhibited favorable pharmacokinetic properties for oral administration and showed better efficacy than 1 in both Pfeiffer and Karpas-422 cell-mediated xenograft mouse models, indicating that it might be a new potential therapeutic candidate for EZH2 mutant cancers.
Reference of 766-11-0, 5-Bromo-2-fluoropyridine is a useful research compound. Its molecular formula is C5H3BrFN and its molecular weight is 175.99 g/mol. The purity is usually 95%.
5-Bromo-2-fluoropyridine is a boronic acid that has been shown to react with iodides and form 5-bromo-2-fluoroiodobenzene. The reaction of 5-bromo-2-fluoropyridine with benzene gives the same product as the reaction with 1,3,5-trioxane. The UV absorption of 5-bromo-2-fluoropyridine is found at 230 nm and 260 nm. It also has an absorption band in the infrared region at 1625 cm−1. Vibrational progressions have been observed for this molecule, which are due to dipole moments and electron density distributions in the molecule.
5-bromo-2-fluoropyridine is used in the synthesis of heteroaromatic and aniline derivatives of piperidines as potent ligands used for vesicular acetylcholine transport. , 766-11-0.