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LDC8201

Chemical Structure : LDC8201

CAS No.: 2411873-31-7

LDC8201 (LDC-8201)

Catalog No.: PC-38640Not For Human Use, Lab Use Only.

LDC8201 is a potent, covalent, wild type-sparing inhibitor of EGFR exon20 insertion mutations, exhibits intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations as well as selectivity over wild type EGFR and within the kinome.

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

    Biological Activity

    LDC8201 is a potent, covalent, wild type-sparing inhibitor of EGFR exon20 insertion mutations, exhibits intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations as well as selectivity over wild type EGFR and within the kinome.
    LDC8201 demonstrated tumor shrinkage in mice engrafted with patient-derived EGFR-H773_V774insNPH mutant cells

    Physicochemical Properties

    M.Wt 486.016
    Formula C28H28ClN5O
    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

    N-(5-(4-chloro-2-(4-(4-methylpiperazin-1-yl)phenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-methylphenyl)acrylamide

    References

    1. Jonas Lategahn, et al. J Med Chem. 2022 Apr 29. doi: 10.1021/acs.jmedchem.1c02080.

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