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Emprumapimod

Chemical Structure : Emprumapimod

CAS No.: 765914-60-1

Emprumapimod (PF-07265803, PF 07265803)

Catalog No.: PC-73415Not For Human Use, Lab Use Only.

Emprumapimod (PF-07265803) is a potent, selective and orally bioavailable inhibitor of p38 MAPK, inhibits LPS-induced IL-6 production in RPMI-8226 cells with IC50 of 0.1 nM.

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

    Biological Activity

    Emprumapimod (PF-07265803) is a potent, selective and orally bioavailable inhibitor of p38 MAPK, inhibits LPS-induced IL-6 production in RPMI-8226 cells with IC50 of 0.1 nM.
    Emprumapimod (PF-07265803) (30 mg/kg, p.o.) inhibited LPS induced IL-6 and TNF-alpha by 91% and 95% in SCID-beige mice.
    Emprumapimod (PF-07265803) (30 mg/kg, BID, PO) inhibited RPMI 8226 tumor growth by 72% as a single agent in MM xenograft models.
    Emprumapimod (PF-07265803) inhibited LPS-induced phosphorylation of p38 in RPMI-8226 xenografts.

    Physicochemical Properties

    M.Wt 473.525
    Formula C24H29F2N5O3
    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-[(2S)-1-amino-4-(dimethylamino)-1-oxobutan-2-yl]-5-(2,4-difluorophenoxy)-1-(2-methylpropyl)indazole-6-carboxamide

    References

    1. Dale Wright, et al. Blood (2006) 108 (11): 3478.

    2. Antoine Muchir, et al. Hum Mol Genet. 2012 Oct 1;21(19):4325-33.

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