R788 disodium (Synonyms: Fostamatinib Disodium Hexahydrate;R 788;R-788) |
| Catalog No.GC11811 |
R788 disodium (R788 Disodium) is the oral prodrug of the active compound R406.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1025687-58-4
Sample solution is provided at 25 µL, 10mM.
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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.
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