Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.
McCoull, William;Boyd, Scott;Brown, Martin R.;Coen, Muireann;Collingwood, Olga;Davies, Nichola L.;Doherty, Ann;Fairley, Gary;Goldberg, Kristin;Hardaker, Elizabeth;He, Guang;Hennessy, Edward J.;Hopcroft, Philip;Hodgson, George;Jackson, Anne;Jiang, Xiefeng;Karmokar, Ankur;Laine, Anne-Laure;Lindsay, Nicola;Mao, Yumeng;Markandu, Roshini;McMurray, Lindsay;McLean, Neville;Mooney, Lorraine;Musgrove, Helen;Nissink, J. Willem M.;Pflug, Alexander;Reddy, Venkatesh Pilla;Rawlins, Philip B.;Rivers, Emma;Schimpl, Marianne;Smith, Graham F.;Tentarelli, Sharon;Travers, Jon;Troup, Robert I.;Walton, Josephine;Wang, Cheng;Wilkinson, Stephen;Williamson, Beth;Winter-Holt, Jon;Yang, Dejian;Zheng, Yuting;Zhu, Qianxiu;Smith, Paul D. research published 《 Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy》, the research content is summarized as follows. Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncol. therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl kinase inhibitors are required to validate this hypothesis. Starting from hits from a DNA-encoded library screen, we optimized an imidazo[1,2-a]pyridine series using structure-based compound design to improve potency and reduce lipophilicity, resulting in a highly selective in vivo probe compound 32. We demonstrated dose-dependent in vivo efficacy and target engagement in Mer- and Axl-dependent efficacy models using two structurally differentiated and selective dual Mer/Axl inhibitors. Addnl., in vivo efficacy was observed in a preclin. MC38 immuno-oncol. model in combination with anti-PD1 antibodies and ionizing radiation.
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%., Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics