1. Apoptosis
  2. Bcl-2 Family

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

Cat. No.: HY-15531 Purity: 99.80%
Handling Instructions

Venetoclax (GDC-0199; ABT-199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM.

For research use only. We do not sell to patients.

Venetoclax Chemical Structure

Venetoclax Chemical Structure

CAS No. : 1257044-40-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 108 In-stock
Estimated Time of Arrival: December 31
100 mg USD 140 In-stock
Estimated Time of Arrival: December 31
200 mg USD 190 In-stock
Estimated Time of Arrival: December 31
500 mg USD 300 In-stock
Estimated Time of Arrival: December 31
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5 g   Get quote  

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Customer Review

    Venetoclax purchased from MCE. Usage Cited in: Translational Cancer Research (TCR). Vol 6, No 4. 2017.

    ABT-199 regulates p53/p21 signaling to induce G2/M phase arrest in DOHH2 cells. Representative blots of CDK1/cdc2, cyclin B1, p21 and p53 in DOHH2 cells treated with ABT-199 at 0.1 and 1 μM for 24 h. β-actin is used as the internal control.

    Venetoclax purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1226-1236.

    ABT-199 inhibits various forms of oncogenic GLI activation.

    Venetoclax purchased from MCE. Usage Cited in: Cancer Cell. 2017 Oct 9;32(4):490-505.e10.

    Immunoblot for BAX, BCL-2, BCL-XL, and MCL-1 from immunoprecipitates of BAX from OCI-AML3 cells treated with Venetoclax (1.25 mM), BTSA1 (1.25 mM), or in combination after 2.5 hr, and western blot detection for BAX, BCL-2, BCL-XL, and MCL-1.

    Venetoclax purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1214-1220.

    Bcl-2 family protein expression is assessed by western blotting in CNE-2 and 5-8F cells after treatment with ABT-199 for 48 h.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Venetoclax (GDC-0199; ABT-199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM.

    IC50 & Target

    Bcl-2

    0.01 nM (Ki)

    Bcl-xL

    48 nM (Ki)

    Bcl-W

    245 nM (Ki)

    In Vitro

    Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC50=4 nM), Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC50=261 nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC50=3 nM) but is much less effective against BCL-XL-BCL-XS (EC50=2.2 μM) or MCL-1-NOXA complexes[1].

    In Vivo

    After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05)[1]. Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days resulted in a significant reduction of leukemic burden (P=0.0048)[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)

    Ethanol : < 1 mg/mL (insoluble)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1515 mL 5.7575 mL 11.5149 mL
    5 mM 0.2303 mL 1.1515 mL 2.3030 mL
    10 mM 0.1151 mL 0.5757 mL 1.1515 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (2.88 mM); Clear solution; Need warming

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming

    References
    Cell Assay
    [1]

    RS4;11 cells are seeded at 50,000 per well in 96-well plates and treated with compounds diluted in half-log steps starting at 1 μM and ending at 0.00005 μM. All other leukemia and lymphoma cell lines are seeded at 15,000-20,000 cells per well in the appropriate medium and incubated with Venetoclax or Navitoclax for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration-response data. Mouse FL5.12-BCL-2 and FL5.12-BCL-XL cells are propagated and assessed. Bak-/- Bax-/- double knockout mouse embryonic fibroblasts are seeded into 96-well microtiter plates at 5,000 cells per well in DMEM supplemented with 10% FBS. Venetoclax (ABT-199) in the same culture medium is added in half-log dilutions starting at 5 μM. The cells are then incubated at 37°C (5% CO2) for 48 h, and the effects on proliferation are determined using Cell TiterGlo reagent[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Nonobese diabetic/severe combined immunodeficient γ (NSG) mice are injected at 6 weeks of age in the tail vein with 150 µL phosphate-buffered saline containing 5×106 luciferase-labeled LOUCY cells. At regular time points, the bioluminescence is measured using the IVIS Lumina II imaging system. At 6 weeks, the cells are engrafted and the mice are randomly divided into 2 groups (with an equal number of males and females in both groups), and the treatment is started on day 0. Mice are treated with Venetoclax (ABT-199) 100 mg/kg body weight or with vehicle via oral gavage for 4 consecutive days. At days 0, 2, and 4 the bioluminescene is measured. Before imaging, the mice are injected intraperitoneally with 200 µL of a 15 mg/mL firefly D-luciferin potassium salt solution and anesthetized by inhalation of 5% isoflurane. The mice are imaged 10 minutes after luciferin injection. The total bioluminescence signal in each mouse is calculated via the region of interest tool (total counts) in the Living Image software.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    868.44

    Formula

    C₄₅H₅₀ClN₇O₇S

    CAS No.

    1257044-40-8

    SMILES

    O=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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.80%

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    Product Name:
    Venetoclax
    Cat. No.:
    HY-15531
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    Venetoclax

    Cat. No.: HY-15531