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SHP394

Chemical Structure : SHP394

CAS No.: 2055757-40-7

SHP394 (SHP-394;SHP 394)

Catalog No.: PC-36038Not For Human Use, Lab Use Only.

SHP394 (SHP-394, SHP 394) is a potent, selective, orally bioavailable inhibitor of SHP2 with IC50 of 23 nM, shows p-ERK inhibition with IC50 of 18 nM in cellular assays.

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    Biological Activity

    SHP394 (SHP-394, SHP 394) is a potent, selective, orally bioavailable inhibitor of SHP2 with IC50 of 23 nM, shows p-ERK inhibition with IC50 of 18 nM in cellular assays.
    SHP394 demonstrates antiproliferation activity in the EGFR amplified human esophageal squamous cell carcinoma cell line KYSE520 (IC50=297 nM), also inhibits Detroit-562 pharyngeal carcinoma cell line in vitro with IC50 of 1.38 uM.
    SHP394 shows high lipophilic efficiency, improved potency and enhanced pharmacokinetic properties.
    SHP394 exhibits efficacy in pharyngeal carcinoma Detroit-562 xenograft model.

    Physicochemical Properties

    M.Wt 470.515
    Formula C20H25F3N6O2S
    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

    6-amino-2-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)thio)pyrimidin-4(3H)-one

    References

    1. Sarver P, et al. J Med Chem. 2019 Jan 28. doi: 10.1021/acs.jmedchem.8b01726.

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