Fostamatinib

SKU: orb1227128

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.

Key Properties

• CAS Number: 1025687-58-4
• MW: 624.4232
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₄FN₆Na₂O₉P
• 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
• Target: Syk
• Solubility: 10 mM in DMSO

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

R788 disodium salt | R935788

Quick Database Links

Gene Symbol

Syk