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JNJ-28312141

Chemical Structure : JNJ-28312141

CAS No.: 885692-52-4

JNJ-28312141 (JNJ 28312141)

Catalog No.: PC-63411Not For Human Use, Lab Use Only.

JNJ-28312141 is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.

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    Biological Activity

    JNJ-28312141 is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.
    JNJ-28312141 shows narrow kinase selectivity profile, also potently inhibits KIT (IC50=5 nM), AXL (12 nM), TRKA (15 nM), FLT3 (30 nM), and LCK (88 nM).
    JNJ-28312141 inhibits CSF-1-induced CSF-1R phosphorylation with IC50 of 5 nM, inhibits CSF-1-dependent proliferation of mouse macrophages and CSF-1-induced expression of MCP-1 by human monocytes with IC50 of 3 nM.
    JNJ-28312141 inhibits the ITD-FLT3-dependent proliferation of MV-4-11 cells with IC50 of 21 nM, inhibits FLT3 ligand-induced FLT3 phosphorylation in recombinant Baf3 cells with IC50 of 76 nM.
    JNJ-28312141 demonstrates potential therapeutic activity in AML, solid tumors and bone metastases in vivo.

    Physicochemical Properties

    M.Wt 460.57
    Formula C26H32N6O2
    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

    4-cyano-N-(5-(1-(2-(dimethylamino)acetyl)piperidin-4-yl)-2',3',4',5'-tetrahydro-[1,1'-biphenyl]-2-yl)-1H-imidazole-2-carboxamide

    References

    1. Manthey CL, et al. Mol Cancer Ther. 2009 Nov;8(11):3151-61.

    2. Illig CR, et al. J Med Chem. 2011 Nov 24;54(22):7860-83.

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