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

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    产品仅用于科学研究,不针对患者销售
    数量: - + 件(库存件)
    InvivoChem目录号 #: V0001
    CAS号码 #: 1257044-40-8纯度 ≥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

    Customer Validation
    InvivoChem产品被CNS顶刊文章引用
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, 597(7874):119-125.
    • Citation of InvivoChem Larotrectinib (V2599) by Cell 2020, 183(5):1202-1218.e25
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, 597(7874):119-125.
    • Citation of InvivoChem Larotrectinib (V2599) by Cell 2020, doi: 10.1016/j.cell.2020.10.016.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Vitrakvi by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem LOXO-101 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem  ARRY-470 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem BMS-582949 (V2668) by Cells 2020, 9(6):1472.
    • Citation of InvivoChem Resveratrol (V0430) by  Arterioscler Thromb Vasc Biol 2020, 40(10):2408
    • Citation of InvivoChem LGK974 /WNT974 (V1353) by  Cancer Cell 2021 Apr 12;39(4):529-547.e7.
    • Citation of InvivoChem V1386 Napabucasin (BBI-608) by J Exp Clin Cancer Res 2021 Oct 13;40(1):319.
    • Citation of InvivoChem S63845 (V2797) by Cell Death and Disease 2020, 11:316.
    • Citation of InvivoChem LGK974 /WNT974 (V1353) by  Cancer Cell 2021 Apr 12;39(4):529-547.e7.
    • Citation of InvivoChem Apiin (V4467) by J Med Chem 2020, 63(15):8338-8358.
    • Citation of InvivoChem V0001 venetoclax by WO2021231323A1
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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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      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

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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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