4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 611225-86-6
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFRL858R/T790M NSCLCs by the conformation constrained strategy was written by Chen, Yang;Yang, Linlin;Qiao, Hui;Cheng, Zhongyu;Xie, Jiahao;Zhou, Wenjuan;Huang, Xin;Jiang, Yaoxuan;Yu, Bin;Zhao, Wen. And the article was included in European Journal of Medicinal Chemistry in 2020.Related Products of 611225-86-6 This article mentions the following:
Studies on the third-generation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFRTKIs) targeting EGFRL858R/T790M mutant remain hotspots, specifically for non-small cell lung cancer(NSCLC) were described. In the current study, a new series of EGFR-TKIs with thieno[3,2-d]pyrimidine derivatives bearing quinolin-2(1H)-ones I (R = 4-fluoro-phenylamino, 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-morpholin-4-ylmethyl-phenylamino, etc.) was designed and synthesized, through conformational constrained strategy from the third generation of EGFR-TKI olmutinib. In vitro structure-activity relationship (SAR) studies indicated that compounds I (R = 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(4-methyl-piperazin-1-ylmethyl)-phenylamino, 4-(4-ethyl-piperazin-1-ylmethyl)-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) exhibited good selective inhibition to EGFRL858R/T790M (IC50 閳?250 nM) over wild type EGFR (IC50 > 10000 nM). The observed selectivity of compounds I (R = 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) (A) was also proved by the computational mol. docking and the cellular thermal shift assay. These compounds I had good growth inhibitory effect on the four tested cancer cell lines. Specifically, I (R = 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) could significantly inhibit the colony formation, wound healing and the expression of p-EGFR and its downstream p-ERK in EGFRL858R/T790M H1975 lung cancer cells. The above finding results suggest that the thieno[3,2-d]pyrimidine compounds, especially compounds A, can selectively target the mutant EGFRL858R/T790M in vitro and at cellular level and may serve as the lead compounds for generating new series of the third generation EGFR-TKIs. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Related Products of 611225-86-6).
4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 611225-86-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics