Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Application In Synthesis of 761446-44-0.
Finlay, M. Raymond V.;Barton, Peter;Bickerton, Sue;Bista, Michal;Colclough, Nicola;Cross, Darren A. E.;Evans, Laura;Floc′h, Nicolas;Gregson, Clare;Guerot, Carine M.;Hargreaves, David;Kang, Xiaoming;Lenz, Eva M.;Li, Xu;Liu, Yi;Lorthioir, Olivier;Martin, Matthew J.;McKerrecher, Darren;McWhirter, Claire;O′Neill, Daniel;Orme, Jonathan P.;Mosallanejad, Arash;Rahi, Amar;Smith, Paul D.;Talbot, Verity;Ward, Richard A.;Wrigley, Gail;Wylot, Marta;Xue, Lin;Yao, Tieguang;Ye, Yang;Zhao, Xiliang research published 《 Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance》, the research content is summarized as follows. The epidermal growth factor receptor (EGFR) harboring activating mutations is a clin. validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including osimertinib, have been approved for clin. use. Resistance to these therapies has emerged due to a variety of mol. events including the C797S mutation which renders third-generation C797-targeting covalent EGFR inhibitors considerably less potent against the target due to the loss of the key covalent-bond-forming residue. We describe the medicinal chem. optimization of a biochem. potent but modestly cell-active, reversible EGFR inhibitor starting point with sub-optimal physicochem. properties. These studies culminated in the identification of compound 12 that showed improved cell potency, oral exposure, and in vivo activity in clin. relevant EGFR-mutant-driven disease models, including an Exon19 deletion/T790M/C797S triple-mutant mouse xenograft model.
761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Application In Synthesis of 761446-44-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics