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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-GNE-431
GNE-431

Chemical Structure : GNE-431

CAS No.: 1433820-83-7

GNE-431 (GNE431)

货号: PC-62888Not For Human Use, Lab Use Only.

GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively.

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

    生物&药学活性

    GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively.
    GNE-431 shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled.
    GNE-431 does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells.
    GNE-431 also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM).
    GNE-431 potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.

    物理化学性质&存储条件

    分子量 564.654
    分子式 C30H32N10O2
    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

    3,4,6,7,8,9-Hexahydro-2-[3-(hydroxymethyl)-4-[8-[(4,5,6,7-tetrahydro-5-methylpyrazolo[1,5-a]pyrazin-2-yl)amino]imidazo[1,2-b]pyridazin-6-yl]-2-pyridinyl]pyrazino[1,2-a]indol-1(2H)-one

    参考文献

    1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907.

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