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Remibrutinib (LOU064)

  Cat. No.:  DC39103   Featured
Chemical Structure
1787294-07-8
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More than 5000 active chemicals with high quality for research!
Field of application
Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1787294-07-8
SMILES: CC1=C(C=C(C=C1NC(=O)C2=C(C=C(C=C2)C3CC3)F)F)C4=C(C(=NC=N4)N)OCCN(C)C(=O)C=C
Formula: C27H27F2N5O3
M.Wt: 507.53
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1. [2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23.
Description: Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
References: [1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1. [2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23.
MSDS
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MSDS_20492_DC39103_1787294-07-8
COA
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Cat. No. Product name Field of application
DC48043 BIIB091 BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM.
DC47717 TAK-020 TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
DC42420 Tolebrutinib Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS).
DC39103 Remibrutinib (LOU064) Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
DC28073 CNX-500 CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
DC11914 Poseltinib Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
DC8358 ONO-4059(Tirabrutinib) ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.
DC9942 GDC-0853(RG7845) GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
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