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PF-06862309

Chemical Structure : PF-06862309

CAS No.: 2067281-52-9

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PF-06862309 (PF-06843195 phosphate ester prodrug)

Catalog No.: PC-49022Not For Human Use, Lab Use Only.

PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.

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

    Biological Activity

    PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.
    PF-06862309 demonstrated robust PK/PD correlation and tumor growth inhibition (TGI) in mouse xenograft models with MDAMB361 and MCF7 cell lines.
    PF-06862309 is a clinical candidate for treating breast cancer patients characterized with ER+ , HER2-, and harboring PIK3CA mutations.

    Physicochemical Properties

    M.Wt 578.446
    Formula C20H26F3N8O7P
    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

    2,2-difluoroethyl (S)-3-((2'-amino-5-fluoro-2-morpholino-[4,5'-bipyrimidin]-6-yl)amino)-3-((phosphonooxy)methyl)pyrrolidine-1-carboxylate

    References

    1. Cheng H, et al. J Med Chem. 2021 Jan 14;64(1):644-661.

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