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DDC-01-163

Chemical Structure : DDC-01-163

CAS No.: 2140806-84-2

DDC-01-163 (EGFR PROTAC)

Catalog No.: PC-38232Not For Human Use, Lab Use Only.

DDC-01-163 is an allosteric EGFR degrader that selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected.

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    Biological Activity

    DDC-01-163 is an allosteric EGFR degrader that selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected.
    DDC-01-163 exhibited an acceptable biochemical potency with an IC50 value of 45 nM against EGFR L858R/T790M.
    DDC-01-163 is also effective against osimertinib-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations.
    The anti-proliferative activity of DDC-01-163 against L858R/T790M EGFR-Ba/F3 cells is enhanced when combined with an ATP-site EGFR inhibitor, Osimertinib.

    Physicochemical Properties

    M.Wt 942.061
    Formula C49H51N9O9S
    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

    [2-(6-(6-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethyl)piperazin-1-yl)pyridin-3-yl)-1-oxoisoindolin-2-yl)-2-phenyl-N-(thiazol-2-yl)acetamide]

    References

    1. Jaebong Jang, et al. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489.

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