现货，R935788 (Fostamatinib disodium)，selleck，美国进口，Syk YZ剂，CAS号: 1025687-58-4，目录号 S2206

R935788 (Fostamatinib disodium) 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) also blocked BCR-mediated Ag presentation, thus broadly interrupting the humoral contributions to T cell-driven autoimmunity. Indeed, oral administration of R935788 (Fostamatinib disodium) 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) reduced total B cell numbers and total Ig concentrations. Interestingly, R935788 (Fostamatinib disodium) 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]

• 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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