《Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Cheng, Meng; Yu, Xufen; Lu, Kaylene; Xie, Ling; Wang, Li; Meng, Fanye; Han, Xiaoran; Chen, Xian; Liu, Jing; Xiong, Yue; Jin, Jian. Recommanded Product: Ethyl 3-bromopropanoate The article mentions the following:
Several epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed and approved by Food and Drug Administration for the treatment of non-small-cell lung cancers, but their efficacy can be compromised by acquired drug resistance conferred by EGFR-mutant variants. Here, we described the discovery of a novel E3 ligase von Hippel-Lindau-recruiting EGFR degrader, MS39 (compound 6), and a first-in-class E3 ligase cereblon-recruiting EGFR degrader, MS154 (compound 10), using the proteolysis targeting chimera technol. These compounds potently induced the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines and effectively suppressed the growth of lung cancer cells compared with the corresponding neg. controls. The global proteomic analyses revealed that the compounds were highly selective for EGFR. Furthermore, both compounds were bioavailable in mouse pharmacokinetic studies, and compound 6 is the first EGFR degrader suitable for in vivo efficacy studies. Overall, we provide a set of well-characterized chem. tools to the research community. The experimental part of the paper was very detailed, including the reaction process of Ethyl 3-bromopropanoate(cas: 539-74-2Recommanded Product: Ethyl 3-bromopropanoate)
Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Recommanded Product: Ethyl 3-bromopropanoateSome of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary