R788 (sodium salt)

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRgamma chains and mediates downstream signaling related to platelet function and inflammation. R788 is a prodrug of R406 (Cay-11422), an inhibitor of Syk (Ki = 30 nM). R788 conversion to the biologically active R406 is catalyzed by the action of alkaline phosphatases present on the apical brush-border of the membranes of intestinal enterocytes. It produces anti-inflammatory and immunomodulating effects by inhibiting Syk-mediated IgG Fcgamma receptor signaling, which prevents activation of mast cells, macrophages, and B cells, as well as related inflammatory responses. R788 has undergone clinical evaluation for efficacy in the treatment of rheumatoid arthritis.Formal Name: 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one, disodium salt. CAS Number: 1025687-58-4. Synonyms: Fostamatinib, NSC 745942, R935788, Tamatinib Fosdium. Molecular Formula: C23H24FN6O9P . 2Na. Formula Weight: 624.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: Methanol: 3 mg/mL. lambdamax: 277, 333 nm. SMILES: COC1=C(OC)C=C(NC2=NC(NC3=NC(N(COP([O-])([O-])=O)C(C(C)(C)O4)=O)=C4C=C3)=C(F)C=N2)C=C1OC.[Na+].[Na+]. InChi Code: InChI=1S/C23H26FN6O9P.2Na/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4,,/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29),,/q,2*+1/p-2. InChi Key: HSYBQXDGYCYSGA-UHFFFAOYSA-L.