1. Apoptosis
  2. Bcl-2 Family
  3. A-1155463

A-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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CAS. Nr. : 1235034-55-5

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Based on 23 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A-1155463 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Dec 19.  [Abstract]

    A-1155463 (1-100 nM; 48 h) dose-dependently induced lethality in PD AML cells.

    A-1155463 purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2020 Jul 16;13(1):95.  [Abstract]

    The viability of DFTL-28776 PDX cells was determined after A-1155463 (0.001-10 μM; 24 h) treatment.

    A-1155463 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 21;10(6):395.  [Abstract]

    U87, U251, H1299, and A549 cells were treated with KPT-330 (1 μM) for 24 h and further with A-1155463 (1 μM; 24 h), then subjected to western blot or flow cytometry analysis for the sub-G1 phase.

    A-1155463 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 21;10(6):395.  [Abstract]

    A-1331852 (1 μM; 48 h). Cell viability was measured by the MTT assay.

    A-1155463 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 21;10(6):395.  [Abstract]

    The mitochondrial membrane potential in U251 cells treated with A-1155463 (1 μM; 24 h) was measured by flow cytometry.

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    Beschreibung

    A-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target[2]

    Bcl-xL

    0.01 nM (Ki)

    Bcl-2

    80 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    DMS-79 EC50
    1.44 μM
    Compound: A-1155463
    Antiproliferative activity against human DMS 79 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human DMS 79 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    EOL1 EC50
    2.25 μM
    Compound: A-1155463
    Antiproliferative activity against human EOL1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human EOL1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    GDM-1 EC50
    1.17 μM
    Compound: A-1155463
    Antiproliferative activity against human GDM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human GDM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    HEL EC50
    0.12 μM
    Compound: A-1155463
    Antiproliferative activity against human HEL harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human HEL harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    HL-60 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human HL-60 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human HL-60 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    KG-1 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human KG-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human KG-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    Kasumi 1 EC50
    0.011 μM
    Compound: A-1155463
    Antiproliferative activity against human Kasumi 1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human Kasumi 1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    ML-2 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human ML-2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human ML-2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    MOLM-13 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human MOLM-13 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human MOLM-13 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    MOLM-16 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human MOLM16 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human MOLM16 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    MOLT-4 EC50
    70 nM
    Compound: 32; A-1155463
    Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay
    Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay
    [PMID: 26988306]
    MOLT-4 EC50
    70 nM
    Compound: A-1155463
    Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    [PMID: 25787766]
    MOLT-4 EC50
    > 5000 nM
    Compound: A-1155463
    Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    [PMID: 25787766]
    MOLT-4 IC50
    6.2 nM
    Compound: A-1155463
    Cytotoxicity against human MOLT-4 cells assessed as cell growth inhibition incubated for 72 hrs
    Cytotoxicity against human MOLT-4 cells assessed as cell growth inhibition incubated for 72 hrs
    [PMID: 35182816]
    MV4-11 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H1048 EC50
    > 10 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H1048 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H1048 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H1417 EC50
    0.007 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H1417 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H1417 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H146 EC50
    0.065 μM
    Compound: 17, A-1155463
    Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum incubated for 48 hrs by Cell titerGlo reagent based assay
    Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum incubated for 48 hrs by Cell titerGlo reagent based assay
    [PMID: 25313317]
    NCI-H1836 EC50
    0.015 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H1836 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H1836 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H187 EC50
    0.18 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H187 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H187 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H211 EC50
    1.35 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H211 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H211 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H345 EC50
    > 10 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H345 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H345 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H446 EC50
    0.2 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H446 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H446 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H69 EC50
    3.2 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H69 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H69 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NCI-H889 EC50
    6.31 μM
    Compound: A-1155463
    Antiproliferative activity against human NCI-H889 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NCI-H889 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    NOMO-1 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human NOMO-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human NOMO-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    OCI-AML-3 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    OCI-AML-5 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human OCI-AML5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human OCI-AML5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    OCI-AML2 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human OCI-AML2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human OCI-AML2 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    Platelet IC50
    7.1 nM
    Compound: A-1155463
    Cytotoxicity against human platelets assessed as cell growth inhibition incubated for 24 hrs
    Cytotoxicity against human platelets assessed as cell growth inhibition incubated for 24 hrs
    [PMID: 35182816]
    RS4-11 EC50
    > 5 μM
    Compound: 32; A-1155463
    Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay
    Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay
    [PMID: 26988306]
    SET-2 EC50
    0.08 μM
    Compound: A-1155463
    Antiproliferative activity against human SET2 harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human SET2 harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    SIG-M5 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human SIG-M5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human SIG-M5 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    SKM-1 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human SKM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human SKM-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    THP-1 EC50
    > 5 μM
    Compound: A-1155463
    Antiproliferative activity against human THP-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    Antiproliferative activity against human THP-1 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
    [PMID: 25787766]
    In Vitro

    A-1155463 shows picomolar binding affinity to BCL-XL (Ki<0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) [2].
    A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS[3].

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

    In Vivo

    A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses[2].

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

    Molekulargewicht

    669.79

    Formel

    C35H32FN5O4S2

    CAS. Nr.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 50 mg/mL (74.65 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 1.4930 mL 7.4650 mL 14.9301 mL
    5 mM 0.2986 mL 1.4930 mL 2.9860 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.

    • Molaritätsrechner

    • Verdünnungsrechner

    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 (3.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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 (3.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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:

    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.
    Reinheit & Dokumentation

    Purity: 99.60%

    Verweise
    Tierverwaltung
    [2]

    Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-1155463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells with a daily dose at 5 mg/kg IP for 14 days[2].

    MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.

    Verweise

    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 1.4930 mL 7.4650 mL 14.9301 mL 37.3251 mL
    5 mM 0.2986 mL 1.4930 mL 2.9860 mL 7.4650 mL
    10 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7325 mL
    15 mM 0.0995 mL 0.4977 mL 0.9953 mL 2.4883 mL
    20 mM 0.0747 mL 0.3733 mL 0.7465 mL 1.8663 mL
    25 mM 0.0597 mL 0.2986 mL 0.5972 mL 1.4930 mL
    30 mM 0.0498 mL 0.2488 mL 0.4977 mL 1.2442 mL
    40 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9331 mL
    50 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7465 mL
    60 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6221 mL
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      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.

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    Produktname:
    A-1155463
    Art. -Nr.:
    HY-19725
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