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  3. Digitoxin

Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .

For research use only. We do not sell to patients.

CAS No. : 71-63-6

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Digitoxin:

Top Publications Citing Use of Products

    Digitoxin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2024 Sep 4:15:1433137.  [Abstract]

    Cell viability was analyzed after indicated treatment for 24 h (Digitoxin (Dig): 1 μΜ; Oua: 1 μΜ).

    Digitoxin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2024 Sep 4:15:1433137.  [Abstract]

    Cell lysates were performed immunoblotting after DDP treatment in the presence or absence of Digitoxin (Dig)/Oua for 24 h.

    Digitoxin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2024 Sep 4:15:1433137.  [Abstract]

    The combination of 3-MA or Digitoxin (Dig) (3 mg/kg, i.p.) with DDP significantly reduced the tumor volume and tumor weight in the mouse xenograft model.

    Digitoxin purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2024 Aug;52(2):103.  [Abstract]

    Transwell assay detected the migration of HCCC9810 and HuCCT1 treated with Digitoxin (DT).

    Digitoxin purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2024 Aug;52(2):103.  [Abstract]

    Digitoxin (DT) could reduce the α2,6 sialylation on the cell membrane, and the overexpression of ST6GAL1 was able to counteract the reduction effect induced by DT by Flow cytometry.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure [1][2][3][4][5].

    IC50 & Target

    Bcl-2

     

    Caspase-9

     

    Caspase 3

     

    Bax

     

    HSV-1

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    Cancer cell lines IC50
    0.1 μM
    Compound: 2
    Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
    Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
    [PMID: 19894733]
    DU-145 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    HCT-116 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    HCT-116 IC50
    0.74 μM
    Compound: 2
    Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
    Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
    [PMID: 19894733]
    HFF CC50
    2.8 μM
    Compound: 1
    Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay
    Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay
    [PMID: 24900847]
    HFF CC50
    6 μM
    Compound: 1
    Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay
    Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay
    [PMID: 24900847]
    HT-29 IC50
    0.068 μM
    Compound: (+)-Digitoxin
    Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    [PMID: 32096998]
    HT-29 IC50
    4.07 μM
    Compound: 2
    Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
    Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
    [PMID: 19894733]
    HT-29 IC50
    67.6 nM
    Compound: Digitoxin
    Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    Hep 3B2 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay
    Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    K562 IC50
    6.4 nM
    Compound: 1
    Cytotoxicity against human K562 cells by XTT assay
    Cytotoxicity against human K562 cells by XTT assay
    [PMID: 16309315]
    KURAMOCHI IC50
    5911 nM
    Compound: Digitoxin
    Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    MCF7 IC50
    0.02 μM
    Compound: 1, DT
    Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay
    Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay
    [PMID: 21421322]
    MCF7 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    MCF7 IC50
    10.2 nM
    Compound: 1
    Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
    Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
    [PMID: 16309315]
    MDA-MB-231 IC50
    0.48 μM
    Compound: (+)-Digitoxin
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    [PMID: 32096998]
    MDA-MB-231 IC50
    482 nM
    Compound: Digitoxin
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    MDA-MB-435 IC50
    0.043 μM
    Compound: (+)-Digitoxin
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    [PMID: 32096998]
    MDA-MB-435 IC50
    43.3 nM
    Compound: Digitoxin
    Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    MDCK IC50
    0.12 μM
    Compound: Digitoxin
    TP_TRANSPORTER: inhibition of Digoxin uptake in OATP4C1-expressing MDCK cells
    TP_TRANSPORTER: inhibition of Digoxin uptake in OATP4C1-expressing MDCK cells
    [PMID: 14993604]
    NCI-H460 GI50
    10.7 nM
    Compound: 1
    Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay
    Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay
    [PMID: 21643465]
    NCI-H460 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    NCI-H460 IC50
    357 nM
    Compound: 1
    Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining
    Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining
    [PMID: 21643465]
    NCI/ADR-RES IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay
    Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    OVCAR-3 IC50
    0.12 μM
    Compound: (+)-Digitoxin
    Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
    [PMID: 32096998]
    OVCAR-3 IC50
    117.1 nM
    Compound: Digitoxin
    Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    OVCAR-4 IC50
    425.6 nM
    Compound: Digitoxin
    Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    OVCAR-5 IC50
    321 nM
    Compound: Digitoxin
    Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    OVCAR-8 IC50
    71.5 nM
    Compound: Digitoxin
    Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    [PMID: 28234008]
    SF-268 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    SK-OV-3 IC50
    0.44 μM
    Compound: digitoxin
    Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay
    Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay
    [PMID: 16309329]
    TK-10 IC50
    3.2 nM
    Compound: 1
    Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
    Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
    [PMID: 16309315]
    UACC-62 IC50
    33.5 nM
    Compound: 1
    Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
    Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
    [PMID: 16309315]
    Vero CC50
    > 50 μM
    Compound: Digitoxin
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    < 0.23 μM
    Compound: Digitoxin
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    In Vitro

    Digitoxin (0-80 nM, 72 h) compromised cell survival in PC12 cells[1].
    Digitoxin (4-1000 nM, 24-48 h) has an antitumor effects in MHCC97H, A549, HCT116 and HeLa cells[3].
    Digitoxin (4-100 nM, 24-48 h) disrupts the cell cycle in HeLa cells[3].
    Digitoxin (20-500 nM, 48 h) activates mitochondrial apoptosis in HeLa cells[3].

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

    Cell Viability Assay[3]

    Cell Line: MHCC97H, A549, HCT116 and HeLa cells
    Concentration: 4-1000 nM
    Incubation Time: 24 h, 48 h
    Result: Dcreased the viability of these cancer cells in a dose- and time-dependent manner, with the IC50 values ranging from 0.075 to 0.395 µM following digitoxin treatment for 24 h and from 0.028 to 0.077 µM following digitoxin treatment for 48 h.

    Cell Cycle Analysis[3]

    Cell Line: HeLa cells
    Concentration: 4 nM, 20 nM, 100 nM
    Incubation Time: 24 h, 36 h, 48 h
    Result: Increased cell population in the G2/M phase from 16.27 to 18.36, 23.46 and 31.51% at concentrations of 20 nM for12, 24 and 36 h.
    Increased average cell population in the G2/M phase from 16.27 to 28.07% at concentrations of 4, 20 and 100 nM for 24 h.
    Significantly decreased the protein expression levels of total CDK1 and phosphorylated CDK1.

    Apoptosis Analysis[3]

    Cell Line: HeLa cells
    Concentration: 20 nM, 100 nM, 500 nM
    Incubation Time: 48 h
    Result: Upregulated Bax expression and unaltered Bcl-2 expression.
    Significantly increased the expression of cytochrome c.
    In Vivo

    Digitoxin (1-2 mg/kg, Intraperitoneal injection, once a day for 19 days) has anticancer effects in nude mice[3].
    Digitoxin (0.3-3 μg/kg, Intraperitoneal injection, once a day for 4 days) blocks the host over-production of cytokines in the cotton rat lung[4].

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

    Animal Model: nude mice harboring HeLa tumor xenografts[3]
    Dosage: 1 mg/kg, 2 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Decreased the tumor volume from 330.71±45.61 to 214.56.93±73.25 mm.
    Strongly increased the protein levels of cleaved caspase-3.
    Reduced the number of Ki-67-positive cells.
    Animal Model: cotton rats[4]
    Dosage: 0.3 μg/kg, 1 μg/kg, 3 μg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Blocked cytokine storm.
    Differentially affected cytokine expression.
    Left immune cell density intact in virus-infected lung.
    Clinical Trial
    Molecular Weight

    764.94

    Formula

    C41H64O13

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O

    Structure Classification
    Initial Source
    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 : 100 mg/mL (130.73 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 1.3073 mL 6.5365 mL 13.0729 mL
    5 mM 0.2615 mL 1.3073 mL 2.6146 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
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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

      Solubility: ≥ 2.5 mg/mL (3.27 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 (3.27 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.
    Purity & Documentation

    Purity: 99.22%

    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 1.3073 mL 6.5365 mL 13.0729 mL 32.6823 mL
    5 mM 0.2615 mL 1.3073 mL 2.6146 mL 6.5365 mL
    10 mM 0.1307 mL 0.6536 mL 1.3073 mL 3.2682 mL
    15 mM 0.0872 mL 0.4358 mL 0.8715 mL 2.1788 mL
    20 mM 0.0654 mL 0.3268 mL 0.6536 mL 1.6341 mL
    25 mM 0.0523 mL 0.2615 mL 0.5229 mL 1.3073 mL
    30 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0894 mL
    40 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8171 mL
    50 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6536 mL
    60 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
    80 mM 0.0163 mL 0.0817 mL 0.1634 mL 0.4085 mL
    100 mM 0.0131 mL 0.0654 mL 0.1307 mL 0.3268 mL
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    • 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.

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    Product Name:
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    Cat. No.:
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