R788 disodium hexahydrate

SKU: orb2655609

Description

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.

Key Properties

• CAS Number: 914295-16-2
• MW: 732.51
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₄FN₆Na₂O₉P.6H₂O
• SMILES: 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+]
• Target: Syk
• Solubility: DMSO: 31.81 mg/mL (Need ultrasonic); H2O: 6.6 mg/mL (Need ultrasonic and warming); H2O: < 6.8 mg/mL

Bioactivity

• 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.

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

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

Quick Database Links

Gene Symbol

Syk