Name: R788 disodium
Price: 145.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    R788, which is the prodrug of R406, is a potnet and selective Syk inhibitor. The spleen tyrosine kinase (Syk) plays a key role in the signaling of activating Fc receptors and the B-cell receptor (BCR).
    In vitro: R406 was found to induce the apoptosis of the majority of examined DLBCL cell lines and could specifically inhibit both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYKdependent phosphorylation of the B-cell linker protein [BLNK]) [1].
    In vivo: R788 effectively inhibits BCR signaling, demonstrating reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated Eμ-TCL1 transgenic mouse. Moreover, the effect of R788 was found to be selective for the malignant clones, since no disturbance in the production of normal B lymphocytes was observed [2].
    Clinical trial: In a phase II clinical trial, R788 treatment effectively improved American College of Rheumatology response rates in patients with eumatoid arthritis [3].
    
    [1] Chen L, Monti S, Juszczynski P, Daley J, Chen W, Witzig TE, Habermann TM, Kutok JL, Shipp MA. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood. 2008 Feb 15;111(4):2230-7.
    [2] Suljagic M, Longo PG, Bennardo S, Perlas E, Leone G, Laurenti L, Efremov DG. The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood. 2010 Dec 2;116(23):4894-905.
    [3] Bajpai M. Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases. IDrugs. 2009 Mar;12(3):174-85.
- Properties
  - Alternative Name
    
    Fostamatinib Disodium Hexahydrate;R 788;R-788; disodium;[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate
    
    CAS Number
    
    1025687-58-4
    
    Molecular Formula
    
    C23H24FN6Na2O9P
    
    Molecular Weight
    
    624.42
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥62.4 mg/mL in DMSO with gentle warming; insoluble in EtOH; ≥2.53 mg/mL in H2O with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

R788 disodium

R788 disodium

Background

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