R406 is an orally available small molecule targeting spleen tyrosine kinase (SYK) inhibitor with IC50 ~40 nM. It can block Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B lymphocytes. R406 has shown efficacy in a number of animal models of immune disorders. R406’s pro-drug R788 (Fostamatinib) is currently in phase III clinical trials to treat rheumatoid arthritis.
Technical information:
| Chemical Formula: | C22H23FN6O5 | |
| CAS #: | 841290-80-0 | |
| Molecular Weight: | 470.45 | |
| Purity: | >98% | |
| Appearance: | Gray solid | |
| Chemical Name: | 6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one | |
| Solubility: | Up to 20 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
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. | Sweeny DJ, Li W, Grossbard E, Lau DT. Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey. Xenobiotica. 2010;40(6):415-23. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
