Syk
Syk, along with Zap-70, is a member of the Syk family of tyrosine kinases. These non-receptor cytoplasmic tyrosine kinases share a characteristic dual SH2 domain separated by a linker domain. While Syk and Zap-70 are primarily expressed in hematopoietic tissues, there is expression of Syk in a variety of tissues. Within B and T cells respectively, Syk and Zap-70 transmit signals from the B-Cell receptor and T-Cell receptor. Syk plays a similar role in transmitting signals from a variety of cell surface receptors including CD74, Fc Receptor, and integrins.
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Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 2.
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ER 27319 maleate是选择性 Syk 激酶抑制剂。
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R406是Syk抑制剂，IC50为41 nM，比对Flt3的抑制性强5倍。
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PRT062607 (P505-15, BIIB057) HCl是一种新型，高度选择性的Syk抑制剂，IC50为1 nM，作用于Syk比作用于Fgr， Lyn， FAK， Pyk2和Zap70选择性高80倍以上。
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Entospletinib是口服有效的Syk抑制剂，IC50为7.7 nM，其临床实验主要针对自身免疫和癌症方面的适应症。
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