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QLT0267

Chemical Structure : QLT0267

CAS No.: 866409-68-9

QLT0267 (QLT-0267)

Catalog No.: PC-49560Not For Human Use, Lab Use Only.

QLT-0267 (QLT0267) is a potent, selective inhibitor of integrin-linked kinase (ILK), inhibits the kinase activity of ILK in cell-free assay at 26 nM.

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    Biological Activity

    QLT-0267 (QLT0267) is a potent, selective inhibitor of integrin-linked kinase (ILK), inhibits the kinase activity of ILK in cell-free assay at 26 nM.
    QLT0267 inhibited cell growth in thyroid cancer cell lines with an mean IC50 of 3 uM.
    QLT0267 inhibits the kinase activity of ILK in cell-free assay at 26 nmol/L and shows 1,000-fold selectivity over other kinases, including CK2, CSK, DNA-PK, PIM1, protein kinase B or AKT kinase, and PKC, 100-fold selectivity over extracellular signal-regulated kinase 1, GSK3β, LCK, PKA, p70S6K, and RSK1.
    QLT0267 inhibits cell growth, proliferation, and induction of apoptosis in thyroid cancer cell lines.
    QLT0267 inhibits epidermal growth factor-induced phosphorylation of AKT in Hth74 cells.
    QLT0267 (50 and 100 mg/kg) induces tumor growth inhibition on DRO thyroid cancer xenografts, inhibits the phosphorylation of AKT and induces apoptosis in vivo.
    QLT0267 also reduces mean vascular density (MVD) of tumor and induces apoptosis of tumor-associated endothelial cells.

    Physicochemical Properties

    M.Wt 232.25
    Formula C10H12N6O
    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-(2-(4-methoxyphenyl)hydrazineylidene)-4H-pyrazole-3,5-diamine

    References

    1. Younes MN, et al. Mol Cancer Ther. 2005 Aug;4(8):1146-56.

    2. Koul D, et al. Mol Cancer Ther. 2005 Nov;4(11):1681-8.

    3. Troussard AA, et al. Cancer Res. 2006 Jan 1;66(1):393-403.

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