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R788 disodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
R788 disodium图片
CAS NO:1025687-58-4
规格:98%
分子量:624.42
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Syk inhibitor,ATP competitive and potent
CAS:1025687-58-4
分子式:C23H24FN6Na2O9P
分子量:624.42
纯度:98%
存储:Store at -20°C

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].


参考文献:
[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.