R406

• CAT Number: I005039
• CAS Number: 841290-81-1
• Molecular Formula: C22H23FN6O5.C6H6O3S
• Molecular Weight: 628.63
• Purity: ≥95%
• Synonyms: benzenesulfonic acid;6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
• Target: Apoptosis
• Solubility: DMSO: ≥ 61 mg/mL
• Storage: 3 years -20C powder
• IC50: 41 nM
• InChI: InChI=1S/C22H23FN6O5.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30);1-5H,(H,7,8,9)
• InChIKey: UXDRJPYSTZHIOE-UHFFFAOYSA-N
• SMILES: CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O

R406（Cat No.:I005039）is a potent and selective inhibitor of spleen tyrosine kinase (Syk), a crucial enzyme in immune cell signaling. By inhibiting Syk, R406 disrupts downstream signaling pathways, including those involved in B-cell receptor (BCR) and Fc receptor-mediated activation, thereby reducing inflammatory cytokine production and immune cell proliferation. R406 is widely used in research on autoimmune diseases, such as rheumatoid arthritis and systemic lupus erythematosus, where excessive immune responses play a role. It is also valuable for studying the modulation of immune responses and potential therapeutic strategies targeting Syk.

Reference

[1]. Braselmann S, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther, 2006, 319(3), 998-1008.
[2]. Quiroga MP, et al. B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406. Blood, 2009, 114(5), 1029-1037.
[3]. Lhermusier T, et al. The Syk-kinase inhibitor R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies. J Thromb Haemost, 2011, 9(10), 2067-2076.
[4]. Zhu Y, et al. Immunotoxicity assessment for the novel Spleen tyrosine kinase inhibitor R406. Toxicol Appl Pharmacol, 2007, 221(3), 268-277.