Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase was written by Angst, Daniela;Gessier, Francois;Janser, Philipp;Vulpetti, Anna;Walchli, Rudolf;Beerli, Christian;Littlewood-Evans, Amanda;Dawson, Janet;Nuesslein-Hildesheim, Barbara;Wieczorek, Grazyna;Gutmann, Sascha;Scheufler, Clemens;Hinniger, Alexandra;Zimmerlin, Alfred;Funhoff, Enrico G.;Pulz, Robert;Cenni, Bruno. And the article was included in Journal of Medicinal Chemistry in 2020.Recommanded Product: 179232-29-2 This article mentions the following:
Bruton’s tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune diseases. The use of currently marketed covalent BTK inhibitors is limited to oncol. indications based on their suboptimal kinase selectivity. We describe the discovery and preclin. profile of LOU064 (remibrutinib, 25), a potent, highly selective covalent BTK inhibitor. LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. It demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. LOU064 is currently being tested in phase 2 clin. studies for chronic spontaneous urticaria and Sjoegren’s syndrome. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Recommanded Product: 179232-29-2).
Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Recommanded Product: 179232-29-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary