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DGY-09-192

Chemical Structure : DGY-09-192

CAS No.: 2504949-52-2

DGY-09-192

Catalog No.: PC-72309Not For Human Use, Lab Use Only.

DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.
    DGY-09-192 exhibited two-digit nanomolar DC50s for both wildtype FGFR2 and several FGFR2-fusions, resulting in degradation-dependent antiproliferative activity in representative gastric cancer and cholangiocarcinoma cells (IC50=1 nM).
    DGY-09-192 induced degradation of a clinically relevant FGFR2 fusion protein in xenograft model.

    Physicochemical Properties

    M.Wt 1017.041
    Formula C49H59Cl2N11O7S
    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,4R)-1-((S)-2-(2-(4-(4-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

    References

    1. Guangyan Du, et al. Angew Chem Int Ed Engl. 2021 Jul 12;60(29):15905-15911.

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