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    Venetoclax (ABT-199; GDC-0199)
    Venetoclax (ABT-199; GDC-0199)

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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 #: V0001
    CAS #: 1257044-40-8Purity ≥98%

    Description: Venetoclax (formerly known as ABT-199 or GDC-0199; Venclexta) is a potent, selective and orally bioavailable small molecule inhibitor of the anti-apoptotic protein BCL-2 (B-cell lymphoma-2) with Ki of<0.01 nM. On April 11, 2016, the FDA approved venetoclax for use in patients with  chronic lymphocytic leukemia (CLL) who have 17p deletion (deletion located on the chromosome 17 short arm) and who have been treated with at least one prior therapy. The mechanism of action of venetoclax is to mimic BH3 (the native ligand of BCL-2) and act as a BCL-2 inhibitor. It blocks the anti-apoptotic BCL-2 protein, leading to programmed cell death of CLL cells.

    References:  2017 Apr;102(4):755-764; Souers AJ, et al. Nat Med, 2013, 19(2), 202-208.


    Publications Citing Use of InvivoChem Venetoclax (ABT-199; GDC-0199)

    [1] Seiller et al. Cell Death and Disease ( 2020) 11:316.

    [2] VCP/p97 inhibitor for the treatment of cancer. WO 2021/231323 A1

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    Molecular Weight (MW)868.44
    FormulaC45H50ClN7O7S
    CAS No.1257044-40-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (115.1 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    SMILES CodeO=C(NS(=O)(C1=CC=C(NCC2CCOCC2)C([N+] ([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC5=C (C6=CC=C(Cl)C=C6)CC(C)(C)CC5)CC4)C=C3OC7=CN=C(NC=C8)C8=C7 
    SynonymsVenclexta; GDC0199; ABT 199; RG7601; GDC0199; ABT-199; RG7601; GDC 0199; ABT199; RG 7601; Venetoclax


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    GeneralABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts.
    Animal modelFemale C.B-17 SCID mice (DoHH2 and Granta-519 xenografts) and female C.B-17 SCID-beige mice (RS4;11 and Toledo xenografts)
    Formulation60% phosal 50 propylene glycol (PG), 30% polyethylene glycol (PEG) 400 and 10% ethanol
    Dosages100 mg/kg
    AdministrationOral gavage
    ReferencesSouers AJ, et al. Nat Med, 2013, 19(2), 202-208.


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

     Venetoclax (ABT-199, GDC-0199)


    Animals with xenograft lymphomas were treated with Torin1 and/or BCL-2 inhibitor, ABT-199.  2017 Apr;102(4):755-764.

    Venetoclax (ABT-199, GDC-0199)


    BH3 profiling predicts sensitivity to TORKi treatment.   2017;102(4):755-764.

     Venetoclax (ABT-199, GDC-0199)


    ABT-199 response in human T-ALL cell lines. 2014, 124(25):3738-47. 

    Venetoclax (ABT-199, GDC-0199)


    ABT-199 sensitivity in a mouse xenograft model of the T-ALL cell line LOUCY.  2014 ;124(25):3738-47.

     Venetoclax (ABT-199, GDC-0199)


    BCL-2 expression and ABT-199 sensitivity in the Lck-Lmo2 transgenic mouse model.  2014 Dec 11;124(25):3738-47.

    Venetoclax (ABT-199, GDC-0199)


    ABT-199 sensitivity in primary human T-ALL patient samples.  2014 Dec 11;124(25):3738-47.

    Venetoclax (ABT-199, GDC-0199)


    ABT-199 in combination with chemotherapeutic agents in human T-ALL cell lines.  2014 Dec 11;124(25):3738-47.

     

    Venetoclax (ABT-199, GDC-0199)


     

    Venetoclax (ABT-199, GDC-0199)


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