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Vecabrutinib

Chemical Structure : Vecabrutinib

CAS No.: 1510829-06-7

Vecabrutinib (SNS 062;SNS062;SNS-062)

Catalog No.: PC-50001Not For Human Use, Lab Use Only.

Vecabrutinib (SNS-062) is a potent, reversible, non-covalent BTK inhibitor with IC50 of 2.9 and 4.4 nM for WT BTK and C481S BTK, respectively.

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    Biological Activity

    Vecabrutinib (SNS-062) is a potent, reversible, non-covalent BTK inhibitor with IC50 of 2.9 and 4.4 nM for WT BTK and C481S BTK, respectively;

    Binds to Tec kinase family members BTK (Kd=0.3 nM) and ITK (Kd=2.2 nM), but not bind EGFR, active in vitro in cells with the C481S mutation;

    Inhibits pBTK in human whole blood with IC50 of 50 nM, demonstrates favorable pharmacokinetic properties, shows potential for overcoming the ibrutinib resistance due to C481S mutantion in BTK.

    Blood Cancer

    Phase 2 Clinical

    Physicochemical Properties

    M.Wt 529.925
    Formula C22H24ClF4N7O2
    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 Room temperature in continental US; may vary elsewhere
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (3R,3'R,4'S)-1'-(6-amino-5-fluoropyrimidin-4-yl)-3-[3-chloro-5-(trifluoromethyl)anilino]-2-oxo[1,3'-bipiperidine]-4'-carboxamide

    References

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