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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-AZD0449
AZD0449

Chemical Structure : AZD0449

CAS No.: 1236666-76-4

AZD0449 (AZD-0449)

货号: PC-49307Not For Human Use, Lab Use Only.

AZD0449 (AZD-0449) is a potent and highly selective JAK1 inhibitor with IC50 of 2.4 nM, displays >50-fold selectivity over TYK2 and JAK2, and no inhibition against JAK3.

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

    生物&药学活性

    AZD0449 (AZD-0449) is a potent and highly selective JAK1 inhibitor with IC50 of 2.4 nM, displays >50-fold selectivity over TYK2 and JAK2, and no inhibition against JAK3.
    AZD0449 inhibited JAK1-dependent signaling, determined by reductions in IL-4-induced STAT6 phosphorylation in human CD4+ T cells with IC50 of 21.4 nM, inhibited IL-13-induced phosphorylation of STAT6- and TSLP-induced production of CCL17.
    AZD0449 dose-dependently inhibited STAT3, STAT5a, and STAT5b phosphorylation in lung tissue from ovalbumin (OVA)-challenged rats.
    AZD0449 also inhibited eosinophilia in the lung and reduced the late asthmatic response, measured as Penh in the OVA rat model.

    物理化学性质&存储条件

    分子量 375.432
    分子式 C21H21N5O2
    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

    5-((5-methyl-2-((3,4,5-trimethylphenyl)amino)pyrimidin-4-yl)amino)benzo[d]oxazol-2(3H)-one

    参考文献

    1. Magnus Nilsson, et al. Drug Des Devel Ther. 2022 Aug 31;16:2901-2917.

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