R788 disodium hexahydrate

Research use only, not for human use.

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.

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; 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.

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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.

Fostamatinib disodium hexahydrate | R 788 disodium hexahydrate | R-788 disodium hexahydrate

Angiogenesis

Syk

Syk

Inflammation/Immunology

Rheumatoid Arthritis

914295-16-2

732.51

C23H24FN6Na2O9P.6H2O

>98% (HPLC)

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

CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)([O-])[O-])C.O.O.O.O.O.O.[Na+].[Na+]

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)

(-20℃)

With Ice Pack

≥ 2 years