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首页-小分子抑制剂&激动剂-Tyrosine Kinase-ITK-PRN694
PRN694

Chemical Structure : PRN694

CAS No.: 1575818-46-0

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PRN694 (PRN-694)

货号: PC-35183Not For Human Use, Lab Use Only.

PRN694 (PRN-694) is a highly selective, potent, covalent inhibitor of interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) with IC50 of 0.3 and 1.4 nM, respectively.

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

    生物&药学活性

    PRN694 (PRN-694) is a highly selective, potent, covalent inhibitor of interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) with IC50 of 0.3 and 1.4 nM, respectively.
    PRN694 also potently inhibits family member TEC (IC50=3.3 nM), weakly inhibits BTK (IC50=17 nM), has no activity against EGFR, ERBB2 and ERBB4 in a panel of 250 kinases.
    PRN694 prevents T-cell receptor- and Fc receptor-induced cellular and molecular activation, inhibits T-cell receptor-induced T-cell proliferation, and blocks proinflammatory cytokine release as well as activation of Th17 cells.
    PRN694 demonstrates inhibitory activity against T-cell prolymphocytic leukemia cells in ex vivo assays.
    PRN694 is a potent inhibitor of Th1 and Th17 differentiation and cytokine production, markedly reduces disease progression in models of colitis.

    物理化学性质&存储条件

    分子量 543.67
    分子式 C28H35F2N5O2S
    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-(Difluoromethyl)-N-[1-[[(2R)-1-(1-oxo-2-propen-1-yl)-2-pyrrolidinyl]methyl]-5-[[[(1S)-1,2,2-trimethylpropyl]amino]methyl]-1H-benzimidazol-2-yl]-2-thiophenecarboxamide

    参考文献

    1. Zhong Y, et al. J Biol Chem. 2015 Mar 6;290(10):5960-78.

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