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PF-06459988

Chemical Structure : PF-06459988

CAS No.: 1428774-45-1

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PF-06459988 (PF 06459988;PF06459988;PF 6459988)

Catalog No.: PC-60296Not For Human Use, Lab Use Only.

PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

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

    Biological Activity

    PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively; exhibist selectivity over wild-type EGFR (IC50>5 uM); shows potential for treatment of EGFR T790M mutation in advanced NSCLC.

    Lung Cancer

    Phase 1 Discontinued

    Physicochemical Properties

    M.Wt 431.88
    Formula C19H22ClN7O3
    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

    1-[(3R,4R)-3-[[[5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]methyl]-4-methoxy-1-pyrrolidinyl]-2-propen-1-one

    References

    1. Cheng H, et al. J Med Chem. 2016 Mar 10;59(5):2005-24.

    2. Planken S, et al. J Med Chem. 2017 Apr 13;60(7):3002-3019.

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