2. Apoptosis Autophagy
  3. Bcl-2 Family Autophagy
  4. Venetoclax

Venetoclax  (Synonyms: ABT-199; GDC-0199; RG7601)

Cat. No.: HY-15531 Purity: 99.95%
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Vénétoclax (ABT-199; GDC-0199) est un inhibiteur de Bcl-2 qui est très puissant, sélectif et biodisponible par voie orale avec un Ki de moins que 0,01 nM. Vénétoclax induit l'autophagie.

Venetoclax (ABT-199; GDC-0199) ist ein hochpotenter, selektiver und oral bioverfügbarer Bcl-2-Inhibitor mit einem Ki von weniger als 0,01 nM. Venetoklax induziert autophagy.

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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 80 In-stock
Solution
10 mM * 1 mL in DMSO USD 80 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 108 In-stock
100 mg USD 140 In-stock
500 mg USD 460 In-stock
1 g USD 730 In-stock
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Customer Review

Based on 152 publication(s) in Google Scholar

Other Forms of Venetoclax:

Venetoclax Related Antibodies

Top Publications Citing Use of Products

148 Publications Citing Use of MCE Venetoclax

WB

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

    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.

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

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

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

    ABT-199 inhibits various forms of oncogenic GLI activation.

    Venetoclax purchased from MedChemExpress. Usage Cited in: Translational Cancer Research. 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.

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].

    IC50 & Target[1]

    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].

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

    Venetoclax Related Antibodies
    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 results in a significant reduction of leukemic burden[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    868.44

    Formula

    C45H50ClN7O7S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : < 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% Ethanol    60% Phosal 50 PG    30% PEG400

      Solubility: 20 mg/mL (23.03 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 5 mg/mL (5.76 mM); Suspended solution; Need ultrasonic and warming and heat to 49°C

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  45% PEG300    5% Tween-80    50% Saline

      Solubility: 10 mg/mL (11.51 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (11.51 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    COA (250 KB) HNMR (220 KB) LCMS (139 KB) Elemental Analysis Report (107 KB)

    Handling Instructions (2659 KB)
    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.

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1515 mL 5.7575 mL 11.5149 mL 28.7873 mL
    5 mM 0.2303 mL 1.1515 mL 2.3030 mL 5.7575 mL
    10 mM 0.1151 mL 0.5757 mL 1.1515 mL 2.8787 mL
    15 mM 0.0768 mL 0.3838 mL 0.7677 mL 1.9192 mL
    20 mM 0.0576 mL 0.2879 mL 0.5757 mL 1.4394 mL
    25 mM 0.0461 mL 0.2303 mL 0.4606 mL 1.1515 mL
    30 mM 0.0384 mL 0.1919 mL 0.3838 mL 0.9596 mL
    40 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
    50 mM 0.0230 mL 0.1151 mL 0.2303 mL 0.5757 mL
    60 mM 0.0192 mL 0.0960 mL 0.1919 mL 0.4798 mL
    80 mM 0.0144 mL 0.0720 mL 0.1439 mL 0.3598 mL
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    Venetoclax Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Venetoclax1257044-40-8ABT-199 GDC-0199 RG7601ABT199ABT 199GDC0199GDC 0199GDC-0199RG7601RG 7601RG-7601Bcl-2 FamilyAutophagyorallybioavailableInhibitorinhibitorinhibit

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