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Fostamatinib

CAT: 0013-GTR19164052-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19164052-01Size:1 g
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Description
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.
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)

Alternative Products

CatalogName
HY-13038A-01Fostamatinib
B2284-10Fostamatinib (R788)
MBS386031-01R788 (Fostamatinib)
MBS8506288-01R7935788 (Fostamatinib)
BUP07893-01Fostamatinib Disodium
CS-EO-02350Fostamatinib d3

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