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RMS-07

Chemical Structure : RMS-07

CAS No.: 2645409-78-3

RMS-07 (RMS07)

Catalog No.: PC-38336Not For Human Use, Lab Use Only.

RMS-07 (RMS 07) is the first potent, selective irreversible covalent inhibitor of Monopolar spindle kinase 1 (MPS1/TTK) with IC50 of 13 nM, Ki of 0.83 nM.

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    Biological Activity

    RMS-07 (RMS 07) is the first potent, selective irreversible covalent inhibitor of Monopolar spindle kinase 1 (MPS1/TTK) with IC50 of 13 nM, Ki of 0.83 nM.
    RMS-07 demonstrated intracellular target engagement with IC50 of 22.4 nM, shows a high selectivity against MAPKAPK2/3, FGFR4, p70S6Kβ (IC50>1 uM).
    RMS-07 induced cell cycle arrest with a prolonged G2/M phase, downregulated cyclin B1, whereas it upregulated p53, p21, and phospho-γH2A.X, enhanced cleaved PARP levels; RMS-07 attenuates cancer cell proliferation.
    RMS-07 and Navitoclax synergistically inhibit hepatocellular carcinoma cell proliferation.

    Physicochemical Properties

    M.Wt 604.759
    Formula C35H40N8O2
    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

    2-{[2-Acrylamido-4-(4-methylpiperazin-1-yl)phenyl]amino}-N-(2,6-diethylphenyl)-5,6-dihydropyrimido[4,5-e]indolizine-7-carboxamide

    References

    1. Ricardo A M Serafim, et al. J Med Chem. 2022 Feb 15.

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