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    sabutoclax
    sabutoclax

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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 #: V0008
    CAS #: 1228108-65-3Purity ≥98%

    Description: Sabutoclax (BI-97C1) is a novel and potent pan-Bcl-2 inhibitor of Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. Sabutoclax is a derivative of apogossypolone. It showed a high binding affinity to Bcl-xL both in NMR binding assay and in ITC assay, with a Kd value of 0.11μM. Sabutoclax also showed better cell membrane permeability than other apogossypolone derivatives. In PC3 cells, sabutoclax inhibited cell growth with EC50 value of 0.13 μM. In human BP3 cell line, sabutoclax induced cell apoptosis with IC50 value of 0.049 μM. In mice bearing M2182 cancer xenografts, administration of sabutoclax significantly reduced the tumor size. At dose of 5 mg/kg, sabutoclax induced near complete tumor growth suppression.

    References: J Med Chem. 2010 May 27;53(10):4166-76.


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    Molecular Weight (MW)700.78
    FormulaC42H40N2O8
    CAS No.1228108-65-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (142.7 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: 54 mg/mL (77 mM)
    Synonyms BI-97C1; BI 97C1; BI97C1


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    GeneralBI-97C1 displays in vivo efficacy in transgenic mice in which Bcl-2 is overexpressed in splenic B-cells and also demonstrates superior single-agent antitumor efficacy in a prostate cancer mouse xenograft model that depends on Mcl-1 for survival
    Animal modelBcl-2 transgenic mice, human prostate cancer xenografts
    FormulationEthanol:Cremophor EL:saline = 10:10:80
    Dosages1 , 3, 5 mg/kg
    Administrationintraperitoneally
    Reference[1] Wei J, et al. J Med Chem, 2010, 53(10), 4166-4176


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

    sabutoclax
    The combination regimen of Sabutoclax and Celecoxib inhibits OSCC tumor growth in athymic nude mice. Oncotarget 6(18):16623-37, 2015

    sabutoclax

    Genetic or pharmacological knockdown of Mcl-1 sensitizes PC to mda-7/IL-24–mediated apoptosis. PNAS, 108 (21), 8785–8790, 2011


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