1. Apoptosis
  2. Bcl-2 Family

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

Cat. No.: HY-15531 Purity: 99.67%
Handling Instructions

ABT-199 is a highly potent, orally bioavailable and Bcl-2-selective inhibitor with Ki of <0.01 nM.

For research use only. We do not sell to patients.
ABT-199 Chemical Structure

ABT-199 Chemical Structure

CAS No. : 1257044-40-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 80 In-stock
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 108 In-stock
100 mg USD 180 In-stock
200 mg USD 288 In-stock
500 mg USD 528 In-stock
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Customer Review

    ABT-199 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.

    ABT-199 purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1226-1236.

    ABT-199 inhibits various forms of oncogenic GLI activation.

    ABT-199 purchased from MCE. Usage Cited in: Haematologica. 2017 Apr;102(4):755-764.

    Knocking out of 4EBPs induces resistance to TORKi treatment. Ramos is transduced with CRISPR-CAS9 vectors targeting both 4EPB1 and 4EBP2 and immunoblotted with the indicated antibodies. 48 h after treatment with AZD8055 or Torin1, 4EBP1/2 double knock-out (Ramos-DKO) and control (Ramos-C) Ramos cells are immunoblotted with antibodies against MCL1 and BCL-XL

    ABT-199 purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.

    ABT-199 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ABT-199 is a highly potent, orally bioavailable and Bcl-2-selective inhibitor with Ki of <0.01 nM.

    IC50 & Target

    Ki: <0.01 nM (Bcl-2), 48 nM (Bcl-xl), 245 nM (Bcl-w), >444 nM (Mcl-1)[1]

    In Vitro

    ABT-199 potently kills FL5.12-BCL-2 cells (EC50=4 nM), 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), 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 100 mg ABT-199/kg for 4 days resulted in a significant reduction of leukemic burden (P=0.0048)[2].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [1]

    ABT-199 is dissolved in DMSO and stored, and then diluted with appropriate media before use[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 ABT-199 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. 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]

    ABT-199 is formulated in 60% phosal 50 propylene glycol, 30% polyethylene glycol 400, and 10% ethanol (Mice)[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 100 mg ABT-199/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

    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

    Solvent & Solubility

    DMSO: ≥ 51 mg/mL

    ABT-199 is prepared in 60% phosal 50 PG, 30% PEG400 and 10% ethanol[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.67%

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    Product Name:
    ABT-199
    Cat. No.:
    HY-15531
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