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R788 disodium

Catalog No.
A8332
Syk inhibitor,ATP competitive and potent
Grouped product items
SizePriceStock Qty
Evaluation Sample
$28.00
In stock
5mg
$105.00
In stock
10mg
$168.00
In stock
50mg
$428.00
In stock
100mg
$713.00
In stock

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Email: [email protected]

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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].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt624.42
Cas No.1025687-58-4
FormulaC23H24FN6Na2O9P
SynonymsFostamatinib Disodium Hexahydrate;R 788;R-788
Solubility≥62.4 mg/mL in DMSO with gentle warming; insoluble in EtOH; ≥2.53 mg/mL in H2O with gentle warming
Chemical Namedisodium;[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
SDFDownload SDF
Canonical SMILESCC1(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.[Na+].[Na+]
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is an inhibitor of Syk with IC50 of 41 nM.
Targets Syk          
IC50 41 nM          

Quality Control

Chemical structure

R788 disodium

Related Biological Data

R788

Related Biological Data

R788