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R788 disodium hexahydrate

Chemical Structure : R788 disodium hexahydrate

CAS No.: 914295-16-2

R788 disodium hexahydrate (Fostamatinib disodium hexahydrate;R 788 disodium hexahydrate;R-788 disodium hexahydrate)

Catalog No.: PC-43350Not For Human Use, Lab Use Only.

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Fostamatinib (R788) disodium hexahydrateis a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM.
Fostamatinib (R788) dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM, inhibits all phosphorylation events downstream of Syk signaling.
Fostamatinib (R788) specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils.
R788 can inhibit local inflammatory injury mediated by immune complexes; reduces immune complex-mediated inflammation in arthritis models.

Physicochemical Properties

M.Wt 732.51
Formula C23H24FN6Na2O9P.6H2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 31.81 mg/mL (Need ultrasonic); H2O: 6.6 mg/mL (Need ultrasonic and warming); H2O: < 6.8 mg/mL

Chemical Name/SMILES

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, hydrate (1:2:6)

References

1. Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

2. Chen L, et al. Blood. 2008 Feb 15;111(4):2230-7.

3. Suljagic M, et al. Blood. 2010 Dec 2;116(23):4894-905.

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