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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-TAS05567
TAS05567

Chemical Structure : TAS05567

CAS No.: 1429038-15-2

TAS05567 (TAS 05567;TAS-05567;TAS-5567)

货号: PC-63503Not For Human Use, Lab Use Only.

TAS05567 (TAS-5567) is a novel potent, selective, orally available Spleen tyrosine kinase (Syk) inhibitor with IC50 of 0.37 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    TAS05567 (TAS-5567) is a novel potent, selective, orally available Spleen tyrosine kinase (Syk) inhibitor with IC50 of 0.37 nM.
    TAS05567 shows >70% inhibition of Syk and 4 other kinases in a panel of 192 kinases, more selective and potent than R406.
    TAS05567 suppresses induction of BLNK phosphorylation by anti-IgM in Ramos cells (IC50=1.8 nM).
    TAS05567 inhibits BCR-dependent signal transduction in Ramos cells, FcγR-mediated TNF-α production in THP-1 cells, and FcεR-mediated histamine release from RBL-2H3 cells.
    TAS05567 suppresses hind-paw swelling in a dose-dependent manner, markedly reduces histopathologic scores in rheumatoid arthritis models.

    物理化学性质&存储条件

    分子量 439.524
    分子式 C21H29N9O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    3-(((3R,4R)-3-aminotetrahydro-2H-pyran-4-yl)amino)-5-((2-(tert-butyl)-7-methyl-2H-indazol-5-yl)amino)-1,2,4-triazine-6-carboxamide

    参考文献

    1. Hayashi H, et al. J Pharmacol Exp Ther. 2018 May 4. pii: jpet.118.248153.

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