1. Apoptosis
    Autophagy
  2. Bcl-2 Family
    Autophagy

ABT-737 

Cat. No.: HY-50907 Purity: 98.38%
Data Sheet SDS Handling Instructions

ABT-737 is a BH3 mimetic inhibitor of Bcl-xLBcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively, and shows no inhibition against Mcl-1, Bcl-B or Bfl-1.

For research use only. We do not sell to patients.
ABT-737 Chemical Structure

ABT-737 Chemical Structure

CAS No. : 852808-04-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 91 In-stock
5 mg USD 60 In-stock
10 mg USD 102 In-stock
50 mg USD 336 In-stock
100 mg USD 480 In-stock
200 mg USD 816 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

    ABT-737 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-737 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ABT-737 is a BH3 mimetic inhibitor of Bcl-xLBcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively, and shows no inhibition against Mcl-1, Bcl-B or Bfl-1.

    IC50 & Target

    EC50: 78.7 nM (Bcl-xL), 30.3 nM (Bcl-2), 197.8 nM (Bcl-w)

    In Vitro

    ABT-737 and ATO inhibits proliferation and induces apoptosis in SGC-7901 and MGC-803 cells in concentration- and time-dependent manner, and shows a synergistic effect. ABT-737 disturbs the binding of B cell lymphoma (Bcl)-2 homologous antagonist killer and Bcl-extra large[1]. ABT-737 induces a BAX/BAK-dependent impairment of maximal O2 consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O2 consumption rate in B-cell lymphoma cells[2]. ABT-737 induces apoptosis and synergizes with chemotherapy,and disrups BCL-2/BAX heterodimerization and induces BAX conformational change in AML cells[3].

    In Vivo

    ABT-737 (50 mg/kg, i.p.) and ATO significantly suppress SGC-7901 xenograft growth, synergistically inhibit tumour growth and induce apoptosis in vivo[1]. ABT-737 suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.2294 mL 6.1468 mL 12.2936 mL
    5 mM 0.2459 mL 1.2294 mL 2.4587 mL
    10 mM 0.1229 mL 0.6147 mL 1.2294 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [3]

    To determine the binding affinity of GST-BCL-2 family proteins to the FITC-conjugated BH3 domain of BIM (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR), FPAs are performed as follows. Briefly, 100 nM of GST-BCL-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. IC50s are determined using GraphPad Prism software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    ABT-737 is dissolved in DMSO.

    Cells are treated with ABT-737, ABT-263, or vehicle (DMSO) for 4 h in XF24 assay medium (6×104 MCF10A cells, see medium composition below) or RPMI 1640 medium (1×106 B-cell lymphoma cells) and apoptosis is analyzed by Annexin-V-binding/PI exclusion or by sub-diploid nuclei determination. FACS analysis is performed on Becton Dickinson FACScan or FACScalibur instruments. Data analysis is performed with CellQuest software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    ABT-737 is dissolved in DMSO, and added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water).

    For intraperitoneal (i.p.) administration, 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%). Mice injected with FD/ΔRaf-1:ER cells are treated with either ABT-737 (20 and 30 mg/kg/mouse every day i.p. for 21 days starting on day 1 post-cell injection (n=9-10 mice per group) or vehicle or left untreated (control); mice injected with human KG-1 cells are treated with 30 mg/kg ABT-737 starting on day 18 post-cell injection. For noninvasive imaging of FD/ΔRaf-1:ER-luc cells, anesthetized mice are injected with 150 mg/kg of D-luciferin and placed for imaging in the In Vivo Imaging System with total imaging time of 2 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    813.43

    Formula

    C₄₂H₄₅ClN₆O₅S₂

    CAS No.

    852808-04-9

    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

    10 mM in DMSO

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

    Purity: 98.38%

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    ABT-737
    Cat. No.:
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