R406

R406 is a potent ATP-competitive inhibitor of spleen tyrosine kinase (Syk, Ki = 30 nM). Through this action, R406 blocks FcepsilonRI-dependent mast cell activation (EC50 = 43 nM) and, at 3 µM, reduces the release of IL-10, -12, and -13 by immune complex-pulsed dendritic cells. R406 is orally available and can reduce immune complex-mediated inflammation. In cancers characterized by over-expression of Syk, R406 can prevent signaling downstream of Syk and induce apoptosis. R406 also inhibits Syk-dependent signaling through c-Jun N-terminal kinase in rheumatoid arthritis synoviocytes, suggesting a therapeutic intervention in this autoimmune disease.Formal Name: 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one. CAS Number: 841290-80-0. Molecular Formula: C22H23FN6O5. Formula Weight: 470.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.5 mg/ml, DMSO: 0.5 mg/ml. lambdamax: 220, 278, 336 nm. SMILES: COC1=C(OC)C=C(NC2=NC(NC3=NC(NC(C(C)(C)O4)=O)=C4C=C3)=C(F)C=N2)C=C1OC. InChi Code: InChI=1S/C22H23FN6O5/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30). InChi Key: NHHQJBCNYHBUSI-UHFFFAOYSA-N.