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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-DZD8586
DZD8586

Chemical Structure : DZD8586

CAS No.: 2662512-15-2

DZD8586 (Birelentinib, DZD 8586)

货号: PC-21570Not For Human Use, Lab Use Only.

Birelentinib (DZD8586) is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.

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

    生物&药学活性

    Birelentinib (DZD8586) is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.
    DZD8586 exhibits good selectivity against multiple kinases was assessed at Eurofins panel with purified enzymes.
    DZD8586 demonstrateS concentration dependent anti-proliferative effects, with similar GI50s among cells carrying different BTK mutations.
    DZD8586 exhibitS potent cell growth inhibition and induced cell death in a variety of cell lines in a panel of DLBCL cell lines.
    DZD8586 (50 mg/kg) exhibitS profound tumor growth inhibition in a dose-dependent manner, and induces tumor regression in both subcutaneous and CNS tumor models.

    物理化学性质&存储条件

    分子量 453.45
    分子式 C23H21F2N5O3
    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

    ((2S,5S)-5-(4-amino-5-(4-(2,3-difluorophenoxy)phenyl)imidazo[5,1-f][1,2,4]triazin-7-yl)tetrahydro-2H-pyran-2-yl)methanol

    参考文献

    1. Yu Bai, et al. Blood (2023) 142 (Supplement 1): 2822.

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