ABT-737 [852808-04-9]

Referentie HY-50907-5mg

Formaat : 5mg

Merk : MedChemExpress

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ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

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ABT-737 Chemical Structure

ABT-737 Chemical Structure

CAS No. : 852808-04-9

This product is a controlled substance and not for sale in your territory.

Based on 46 publication(s) in Google Scholar

Other Forms of ABT-737:

  • ABT-737-d8 Obtenir un devis

    ABT-737 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Oct 1;461:102-111.  [Abstract]

    Expression of active (cleaved) PARP and active (cleaved) Caspase-3 after 48h of treatment with AGS, 1 μM ABT-737 or 1 μM ABT-737 added to AGS as determined by Western blot. Floating cells are included in lysate.

    Voir tous les produits spécifiques à Isoform Bcl-2 Family:

    Voir toutes les isoformes
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim
    Description

    ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research[1][2][3].

    IC50 & Target[1]

    Bcl-2

    30.3 nM (EC50)

    Bcl-xL

    78.7 nM (EC50)

    Bcl-W

    197.8 nM (EC50)

    Bcl-B

    1820 nM (EC50)

    Bfl-1

    >10 μM (EC50)

    Mcl-1

    >10 μM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    CCRF-CEM IC50
    0.74 μM
    Compound: 1, ABT-737
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    DU-145 IC50
    27.6 μM
    Compound: 7, ABT-737
    Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    FL5.12 EC50
    30 nM
    Compound: 1, ABT-737
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum
    [PMID: 18841882]
    FL5.12 EC50
    7.7 nM
    Compound: 1, ABT-737
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum
    [PMID: 18841882]
    HCT-116 IC50
    4.06 μM
    Compound: 7, ABT-737
    Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    HCT-116 IC50
    47.7 μM
    Compound: ABT-737
    Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    HL-60 IC50
    0.76 μM
    Compound: 1, ABT-737
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    HL-60 IC50
    0.97 μM
    Compound: ABT-737
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    Jurkat IC50
    1.38 μM
    Compound: 7, ABT-737
    Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    K562 IC50
    16.4 μM
    Compound: ABT-737
    Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry
    Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry
    [PMID: 23314054]
    K562 IC50
    34.7 μM
    Compound: 1, ABT-737
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    Leukemia cell IC50
    > 1 μM
    Compound: 1, ABT-737
    Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay
    Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay
    [PMID: 23767404]
    Leukemia cell IC50
    > 10 μM
    Compound: 1, ABT-737
    Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay
    Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay
    [PMID: 23767404]
    MCF7 IC50
    21.26 μM
    Compound: 7, ABT-737
    Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    MCF7 IC50
    25.33 μM
    Compound: ABT-737
    Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
    Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    MCF7 EC50
    4.39 μM
    Compound: ABT-737
    Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 35421577]
    MDA-MB-435 IC50
    > 122.94 μM
    Compound: ABT-737
    Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    MEF EC50
    > 10000 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum
    [PMID: 21366295]
    MEF EC50
    > 10000 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum
    [PMID: 21366295]
    MEF EC50
    0.013 μM
    Compound: 1; ABT-737
    Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis
    Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis
    [PMID: 33904752]
    MEF EC50
    2.03 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum
    [PMID: 21366295]
    MEF EC50
    51 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum
    [PMID: 21366295]
    MEF EC50
    51 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum
    [PMID: 21366295]
    MOLT-4 IC50
    227 nM
    Compound: ABT-263
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    NCI-H1417 IC50
    0.13 μM
    Compound: 1, ABT-737
    Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay
    Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay
    [PMID: 22448988]
    NCI-H1417 IC50
    173.4 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1417 IC50
    412 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H146 EC50
    0.087 μM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum
    Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum
    [PMID: 18841882]
    NCI-H146 IC50
    0.097 μM
    Compound: 1, ABT-737
    Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay
    Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay
    [PMID: 22448988]
    NCI-H146 IC50
    37 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H146 IC50
    43.8 nM
    Compound: ABT-263
    Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    NCI-H187 IC50
    137.7 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1963 IC50
    54 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1963 IC50
    59 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H23 IC50
    71.16 μM
    Compound: ABT-737
    Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay
    Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    NCI-H460 IC50
    8.03 μM
    Compound: 7, ABT-737
    Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    Platelet IC50
    242 nM
    Compound: ABT-263
    Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    Raji IC50
    93.49 μM
    Compound: ABT-737
    Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    RS4-11 IC50
    0.27 μM
    Compound: ABT-737
    Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry
    Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry
    [PMID: 23314054]
    RS4-11 IC50
    0.33 μM
    Compound: ABT-737
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 29453135]
    RS4-11 IC50
    49 nM
    Compound: ABT-263
    Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    SK-OV-3 IC50
    46.59 μM
    Compound: ABT-737
    Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay
    Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    SU.86.86 IC50
    4.24 μM
    Compound: 7, ABT-737
    Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    U-266 IC50
    27.35 μM
    Compound: ABT-737
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    In Vitro

    ABT-737 binds BCL-2, BCL-XL, and BCL-W with high affinity (Ki<1 nM) but binds weakly (Ki>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-XL and BCL-2[1].
    ABT-737 (100 nM; 1-72 hours) induces apoptosis and synergizes with chemotherapy in HL-60 cells[1].
    ABT-737 (5, 7.5, 10 μM; 72 hours) causes approximately 80% HCT116 cell death. The BAX knockout variant is completely resistant to ABT-737[1].
    ABT-737 has no effect on cell cycle distribution. ABT-737 disrupts BCL-2/BAX heterodimerization and induces BAX conformational change in HL-60 leukemic cells[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[3].

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

    In Vivo

    ABT-737 (20, 30 mg/kg/day; i.p.; for 21 days) suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively, in four- to six-week-old CB.17 Scid mice with human leukemia KG-1 cells[1].
    ABT-737 significantly extends survival of mice in this aggressive leukemia model[1].

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

    Masse moléculaire

    813.43

    Formule

    C42H45ClN6O5S2

    CAS No.

    852808-04-9

    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    CN(CC[C@@H](NC1=CC=C(C=C1[N+]([O-])=O)S(NC(C2=CC=C(C=C2)N3CCN(CC3)CC4=CC=CC=C4C5=CC=C(C=C5)Cl)=O)(=O)=O)CSC6=CC=CC=C6)C

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 50 mg/mL (61.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: 2.5 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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.
    Pureté et documentation

    Purity: 99.96%

    Références
    • [1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88.  [Content Brief]

      [2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81.  [Content Brief]

      [3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3.  [Content Brief]

    Essai de kinase
    [1]

    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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    Test cellulaire
    [3]

    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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    Administration animale
    [1]

    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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    Références
    • [1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88.  [Content Brief]

      [2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81.  [Content Brief]

      [3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3.  [Content Brief]

    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 1.2294 mL 6.1468 mL 12.2936 mL 30.7341 mL
    5 mM 0.2459 mL 1.2294 mL 2.4587 mL 6.1468 mL
    10 mM 0.1229 mL 0.6147 mL 1.2294 mL 3.0734 mL
    15 mM 0.0820 mL 0.4098 mL 0.8196 mL 2.0489 mL
    20 mM 0.0615 mL 0.3073 mL 0.6147 mL 1.5367 mL
    25 mM 0.0492 mL 0.2459 mL 0.4917 mL 1.2294 mL
    30 mM 0.0410 mL 0.2049 mL 0.4098 mL 1.0245 mL
    40 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7684 mL
    50 mM 0.0246 mL 0.1229 mL 0.2459 mL 0.6147 mL
    60 mM 0.0205 mL 0.1024 mL 0.2049 mL 0.5122 mL
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    ABT-737852808-04-9ABT737ABT 737Bcl-2 FamilyApoptosisAutophagyMitophagyMitochondrial AutophagyBH3mimeticBCL-2/BAXBIMAMLHL-60HCT116Inhibitorinhibitorinhibit

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