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TAS05567

CAS No. : 1429038-15-2

MCE 站：TAS05567

产品活性：TAS05567 是一种有效的，高选择性，ATP 竞争性和口服活性 Syk 抑制剂，IC₅₀ 为 0.37 nM。在 192 种激酶中，TAS05567 仅显示出对 Syk 和其他 4 种激酶 (FLT3，JAK2，KDR 和 RET 的 IC₅₀ 分别为 10 nM，4.8 nM，600 nM 和 29 nM) 的抑制作用。TAS05567 可用于体液免疫介导的炎症，例如自身免疫性疾病和过敏性疾病。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk

In Vitro: When Ramos cells (human B lymphoma cells) are pretreated with TAS05567 prior to BCR cross-linking by exposure to anti-IgM, there is marked inhibition of the phosphorylation of BLNK, an adaptor protein phosphorylated by activated Syk. The IC₅₀ of TAS05567 for suppressing induction of BLNK phosphorylation by anti-IgM is 1.8 nM. TAS05567 also inhibits PLCγ2 (IC₅₀ of 23 nM) and Erk1/2 (IC₅₀ of 9.8 nM), after stimulation of Ramos cells with anti-IgM.
TAS05567 shows concentration-dependent inhibition of TNF-α production by THP-1 cells stimulated with IgG.
TAS05567 suppresses both calcium flux (IC₅₀ of 27 nM) and histamine release (IC₅₀ of 13 nM) induced by cross-linking of FcεRI with IgE and antigen.
TAS05567 inhibits the formation of mature osteoclasts in a concentration-dependent manner, and osteoclast differentiation is completely suppressed at 30 nM.

In Vivo: TAS05567 (10-30 mg/kg; oral administration; daily; for 9 days; female BALB/c mice) treatment suppresses hind-paw swelling in a dose-dependent manner. The serum MMP-3 levels are significantly lower in both the 10 mg/kg and 30 mg/kg TAS05567 groups than in the vehicle group.

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