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PF-06843195

Chemical Structure : PF-06843195

CAS No.: 2067281-51-8

PF-06843195 (PF06843195)

Catalog No.: PC-49021Not For Human Use, Lab Use Only.

PF-06843195 is a potent, selective PI3Kα inhibitor with Ki value of <0.018 nM, IC50 of 18 nM (RAT1 PI3Kα), with cellular isoform selectivity of 20-fold over PI3Kβ and 9-fold over PI3Kδ.

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

    Biological Activity

    PF-06843195 is a potent, selective PI3Kα inhibitor with Ki value of <0.018 nM, IC50 of 18 nM (RAT1 PI3Kα), with cellular isoform selectivity of 20-fold over PI3Kβ and 9-fold over PI3Kδ.
    PF-06843195 also demonstrated high selectivity over mTOR.
    PF-06843195 is a potent inhibitor of both PI3Kα (Ki< 0.018 nM) and PI3Kδ (Ki< 0.28 nM), but found to be 9-fold selective for PI3Kα over PI3Kδ in cell assays.
    PF-06843195 is selective over two other members of the class I catalytic PI3K kinase group, PI3Kβ and PI3Kγ, >100- and >10 000-fold, respectively, in biochemical assays and 20-fold selective over PI3Kβ in cell assays.

    Physicochemical Properties

    M.Wt 498.467
    Formula C20H25F3N8O4
    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 (3S)-3-{[2'-amino-5-fluoro-2-(morpholin-4-yl)-4,5'-bipyrimidin-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate

    References

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

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