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    UMI-77
    UMI-77

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0009
    CAS #: 518303-20-3Purity ≥98%

    Description: UMI-77 (UMI 77; UMI77) is a novel, potent and selective Mcl-1 (Myeloid cell leukemia-1) inhibitor with Ki of 490 nM. Myeloid cell leukemia-1 (Mcl-1) is a member of the prosurvival Bcl-2 family and is a potent anti-apoptotic protein. Mcl-1 acts as an important survival factor in a broad range of human cancers. As a small-molecule Mcl-1 inhibitor, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein in FP-based binding assays, with Ki value of 0.49μM and bound to the BH3 binding pocket of Mcl-1 protein. UMI-77 bound to A1/Bfl-1, Bcl-w, Bcl-2 and Bcl-xL with Ki values of 5.33, 8.19, 23.83 and 32.99μM. In a pull-down assay, UMI-77 at 10 μM effectively and dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1.

    Reference: Mol Cancer Ther. 2014 Mar;13(3):565-75.  


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    Molecular Weight (MW)468.34
    FormulaC18H14BrNO5S2
    CAS No.518303-20-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 93 mg/mL (198.6 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: Not available
    Solubility (In vivo)5% DMSO+30% PEG 300+dd H2O: 6 mg/mL


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    GeneralIn a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg i.v.) exhibits single-agent antitumor activity without any damage normal tissues
    Animal modelFemale BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells.
    FormulationObatoclax (tartrate salt) is formulated in 9.6% PEG300, 0.4% polysorbate 20, and 5% dextrose; while for the 4T1 tumor model, Obatoclax is formulated  in 9.48% PEG, 0.38% polysorbate 20.
    Dosages0.0313, 0.25, 0.5 and 2 mg/kg
    AdministrationIntravenously (tail vein) once a day
    References[1] Abulwerdi F, et al. Mol Cancer Ther. 2014, 13(3), 565-575.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    UMI-77

    UMI77 disrupts the Mcl-1/Bak complex. Panc-1 (A) and BxPC-3 (B) cells were treated with the indicated concentrations of UMI77 for 48 hours and then prepared for immunoprecipitation and immunoblotting. Mcl-1 was immunoprecipitated from cell lysates and the levels of Bak interacting with Mcl-1 were detected by immunoblotting for Bak. Translational oncology 8(1):47-54, 2015
    UMI-77
    Downregulation of Mcl-1 by siRNA in BxPC-3 cells blocks growth inhibition and apoptosis induced by 2 (UMI-77). Mol Cancer Ther. 2014 Mar;13(3):565-75
    UMI-77
    Inhibition of Mcl-1 by UMI77 does not radiosensitize normal cells. CCL-241 normal small intestinal cells were treated with UMI77 (1-3μM) as illustrated (Figure 3A) and radiosensitization was assessed by clonogenic survival. Translational oncology 8(1):47-54, 2015


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