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    BI-4464
    BI-4464

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4437
    CAS #: 1227948-02-8Purity ≥98%

    Description: BI-4464 is a novel, potent and highly selective ATP competitive inhibitor of PTK2/FAK with an IC50 of 17 nM. IT is a PTK2 ligand used for PROTAC. Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several reports have linked PTK2 depletion and/or pharmacological inhibition to reduced tumorigenicity. However, the clinical relevance of targeting PTK2 still remains to be proven. It is a highly selective and functional PTK2 proteolysis-targeting chimera utilizing von Hippel-Lindau and cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 (cereblon-based) degrades PTK2 with a median DC50 of 30 nM to >80% across a panel of 11 HCC cell lines. Despite effective PTK2 degradation, these compounds did not phenocopy the reported antiproliferative effects of PTK2 depletion in any of the cell lines tested.  

    References: J Med Chem. 2019 Mar 14;62(5):2508-2520.


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    BI-4464

    Molecular Weight: 555.55
    Formula: C₂₈H₂₈F₃N₅O₄
    CAS No.: 1227948-02-8
    SMILES: O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(C(F)(F)F)C(OC4=CC=CC(CC5)=C4C5=O)=N3)C(OC)=C2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationBI-4464; ;BI 4464; BI4464


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