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R788 (Fostamatinib disodium) | Orally active Syk inhibitor

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Price:
$169.00
Catalog #:
C7788-5
Quantity:


Product Description

R788 is an orally-available, ATP-competitive, methylene phosphate prodrug of R406, which is a potent inhibitor of Syk (IC50 = 41 nM). [1] In a broad panel of receptor, ion channel, and enzyme binding assays, R406 was shown to inhibit adenosine A3 receptor (IC50 = 81 nM), adenosine transporter (IC50 = 1.8 uM), and monoamine transporter (IC50 = 2.7 uM). Followup measurements for ligand-induced guanosine 5'-O-(thiotriphosphate) binding to the adenosine A3 receptor showed that R406 possesses antagonistic activity with an IC50 of 93 nM. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 does not inhibit phosphorylation of Sky tyrosine 352, but does inhibit phosphorylation of LAT tyrosine 191. R406 also inhibits IgE- and IgG-mediated activation of Fc receptor signaling.

In a large panel of diffuse large B-cell lymphoma cell lines, R406 inhibited cellular proliferation at EC50s ranging from 0.8 to 8.1 uM. [2]


Technical information:

Chemical Formula:   C23H24FN6O9P.2Na
CAS #:   1025687-58-4
Molecular Weight:   624.42
Purity:   >98%
Appearance:   White
Chemical Name:   2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-, sodium salt (1:2)
Solubility:   Up to 100 mM in DMSO
Synonyms:   Fostamatinib disodium, Fostamatinib, R788, R935788

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Braselmann et al., R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J. Pharma. Exp. Ther. 2006, 319(3), 998-1008. Pubmed ID: 16946104
2. Chen et al., SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 2008, 111, 2230-2237. Pubmed ID: 18006696

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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