tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Product Details of 4248-19-5
Dragovich, Peter S.; Pillow, Thomas H.; Blake, Robert A.; Sadowsky, Jack D.; Adaligil, Emel; Adhikari, Pragya; Bhakta, Sunil; Blaquiere, Nicole; Chen, Jinhua; dela Cruz-Chuh, Josefa; Gascoigne, Karen E.; Hartman, Steven J.; He, Mingtao; Kaufman, Susan; Kleinheinz, Tracy; Kozak, Katherine R.; Liu, Liang; Liu, Liling; Liu, Qi; Lu, Ying; Meng, Fanwei; Mulvihill, Melinda M.; O′Donohue, Aimee; Rowntree, Rebecca K.; Staben, Leanna R.; Staben, Steven T.; Wai, John; Wang, Jian; Wei, BinQing; Wilson, Catherine; Xin, Jianfeng; Xu, Zijin; Yao, Hui; Zhang, Donglu; Zhang, Hongyan; Zhou, Hao; Zhu, Xiaoyu published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties》.Product Details of 4248-19-5 The article contains the following contents:
The biol. and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and related chimeric mols. that effect intracellular degradation of target proteins via ubiquitin ligase-mediated ubiquitination continue to grow. However, these chimeric entities are relatively large compounds that often possess mol. characteristics, which may compromise oral bioavailability, solubility, and/or in vivo pharmacokinetic properties. We therefore explored the conjugation of such mols. to monoclonal antibodies using technologies originally developed for cytotoxic payloads so as to provide alternate delivery options for these novel agents. In this report, we describe the first phase of our systematic development of antibody-drug conjugates (ADCs) derived from bromodomain-containing protein 4 (BRD4)-targeting chimeric degrader entities. We demonstrate the antigen-dependent delivery of the degrader payloads to PC3-S1 prostate cancer cells along with related impacts on MYC transcription and intracellular BRD4 levels. These experiments culminate with the identification of one degrader conjugate, which exhibits antigen-dependent antiproliferation effects in LNCaP prostate cancer cells. In the experiment, the researchers used tert-Butyl carbamate(cas: 4248-19-5Product Details of 4248-19-5)
tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Product Details of 4248-19-5
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