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Fostamatinib

Fostamatinib (R788 disodium salt) 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; dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM, inhibits all phosphorylation events downstream of Syk signaling; 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. Rheumatoid Arthritis Phase 3 Clinical (In Vivo) :Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC0-16 hrs= 10618 ng*h/mL and 30650 ng*h/mL respectively; Cmax=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour) ; t1/2=4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406.

Product Specifications

CAS Number

1025687-58-4

Product Name Alternative

R788 disodium salt | R935788

Field of Research

Pharmacology & Drug Discovery

Purity

>98% (HPLC)

Solubility

10 mM in DMSO

Smiles

[Na+].[Na+].COC1=CC (NC2=NC=C (F) C (NC3=NC4=C (OC (C) (C) C (=O) N4COP ([O-]) ([O-]) =O) C=C3) =N2) =CC (OC) =C1OC

Molecular Formula

C23H24FN6Na2O9P

Molecular Weight

624.4232

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Other Product Names

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)

Available Sizes

Frequently Asked Questions

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