现货,R935788 (Fostamatinib disodium, R788),CAS号:1025687-58-4,美国进口,受体酪氨酸激酶(RTK) ,Syk 抑制剂,selleck,目录号: S2206

信号转导通路: 受体酪氨酸激酶(RTK) >> Syk >> Syk 抑制剂 >> R935788 (Fostamatinib disodium, R788)http://selleck.cn/R935788-Fostamatinib-disodium-S2206.html

技术数据:

分子量(MW): 624.42

化学式:

C23H24FN6O9P.2Na

 

溶解度: DMSO <1mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1025687-58-4

生物活性

 

 

R935788 (Fostamatinib disodium, R788) is a selective Syk inhibitor with an IC50 of 41 nM.R935788 (Fostamatinib disodium) has shown clinical activity in heavily pre-treated NHL and CLL patients, exhibits inhibitory activity against SYK but also inhibits a broad spectrum of other kinase targets. In addition to blocking FcγR-mediated events,R935788 (Fostamatinib disodium, R788) also blocked BCR-mediated Ag presentation, thus broadly interrupting the humoral contributions to T cell-driven autoimmunity. Indeed, oral administration of R935788 (Fostamatinib disodium, R788) significantly delayed spontaneous diabetes onset in NOD mice and successfully delayed progression of early-established diabetes even when treatment was initiated after the development of glucose intolerance. At the DC level, R788 treatment was associated with reduced insulin-specific CD8 priming and decreased DC numbers. At the B cell level, R935788 (Fostamatinib disodium, R788) reduced total B cell numbers and total Ig concentrations. Interestingly, R935788 (Fostamatinib disodium, R788) increased the number of IL-10–producing B cells, thus inducing a tolerogenic B cell population with immunomodulatory activity. Taken together, Syk in APCs is an attractive target in T cell-mediated autoimmune diseases such as type 1 diabetes. [1][2][3][4]

 

 

 

参考文献

Fostamatinib, a Syk-kinase inhibitor, does not affect methotrexate pharmacokinetics in patients with rheumatoid arthritis. Baluom M et al. J Clin Pharmacol. 2011 Jan 5.;

The Syk kinase as a therapeutic target in leukemia and lymphoma. Efremov DG et al. Expert Opin Investig Drugs. ;

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. Suljagic M et al. Blood. 2010 Dec 2.;116(23):4894-905.

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