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DZD8586

Chemical Structure : DZD8586

CAS No.: 2662512-15-2

DZD8586 (Birelentinib, DZD 8586)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 453.45
    Formula C23H21F2N5O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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