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DDC-03-024-01

Chemical Structure : DDC-03-024-01

CAS No.: 2375107-27-8

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DDC-03-024-01

Catalog No.: PC-73295Not For Human Use, Lab Use Only.

DDC-03-024-01 is a potent, mutant-selective allosteric inhibitor of EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 of 10 nM.

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

    Biological Activity

    DDC-03-024-01 is a potent, mutant-selective allosteric inhibitor of EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 of 10 nM.
    DDC-03-024-01 displays no significant activity aginst WT EGFR (IC50>1000 nM) and high selectivity by kinome profiling.
    Cotreatment with cetuximab resulted in antiproliferative activity in EGFR mutant Ba/F3 cells (IC50=0.36 uM, L858R/T790M).

    Physicochemical Properties

    M.Wt 508.597
    Formula C31H29FN4O2
    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

    10-benzyl-8-fluoro-2-(4-(4-methylpiperazin-1-yl)phenoxy)-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one

    References

    1. Dries J H De Clercq, et al. ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553.

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