BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING

    公开(公告)号:CA2668286C

    公开(公告)日:2014-09-16

    申请号:CA2668286

    申请日:2007-11-05

    Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use. The invention relates to a Btk activity probe comprising a Btk inhibitor moiety, a reporter moiety, and a linker moiety that links the inhibitor moiety to the reporter moiety. Specifically described are a Btk inhibitor moiety which covalently bonds to a cysteine residue of a Btk enzyme, a fluorophore and a linker moiety that links the inhibitor moiety to the fluorophore. In an embodiment, the Btk activity probe is: (see compound 3)

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