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CCT-251455

Chemical Structure : CCT-251455

CAS No.: 1400284-80-1

CCT-251455 (CCT 251455;CCT251455)

Catalog No.: PC-61144Not For Human Use, Lab Use Only.

CCT-251455 is a potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).

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    Biological Activity

    CCT-251455 is a potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).
    CCT-251455 stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding.
    CCT-251455 inhibits HCT116 cell growth with GI50 of 0.16 uM, dose-dependently inhibits MPS1 in HCT116 human tumor xenograft model.

    Physicochemical Properties

    M.Wt 503.991
    Formula C26H26ClN7O2
    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

    tert-Butyl 6-(2-Chloro-4-(1-methyl-1H-imidazol-5-yl) phenylamino)-2-(1-methyl-1H-pyrazol-4-yl)-1Hpyrrolo[3,2-c]pyridine-1-carboxylate

    References

    1. Naud S, et al. J Med Chem. 2013 Dec 27;56(24):10045-65.

    2. Gurden MD, et al. Cancer Res. 2015 Aug 15;75(16):3340-54.

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