Lanraplenib

Lanraplenib is an inhibitor of spleen tyrosine kinase (Syk, IC50 = 6.2 nM). It is selective for Syk over a panel of 395 kinases but does inhibit JAK2 (IC50 = 120 nM). Lanraplenib reduces anti-IgM- and anti-CD40-induced proliferation of isolated human B cells (EC50 = 108 nM). It also inhibits immune complex-induced production of TNF-alpha, IL-1beta, and IL-6 in human macrophages (EC50s = 180, 90, and 700 nM, respectively). It reduces proteinuria and increases survival in the NZBWF1 mouse model of systemic lupus erythematosus (SLE).Formal Name: 6-(6-amino-2-pyrazinyl)-N-[4-[4-(3-oxetanyl)-1-piperazinyl]phenyl]-imidazo[1,2-a]amine. CAS Number: 1800046-95-0. Synonyms: GS-9876, GS-SYK. Molecular Formula: C23H25N9O. Formula Weight: 443.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 40 mg/ml, sonicated. SMILES: NC1=NC(C2=CN3C=CN=C3C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=CN=C1. InChi Code: InChI=1S/C23H25N9O/c24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18/h1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29). InChi Key: XCIGZBVOUQVIPI-UHFFFAOYSA-N.