2. Apoptosis Metabolic Enzyme/Protease
  3. MDM-2/p53 E1/E2/E3 Enzyme
  4. Nutlin-3

Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

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CAS 番号 : 548472-68-0

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 105 在庫あり
Solution
10 mM * 1 mL in DMSO USD 105 在庫あり
Solid
5 mg $82 在庫あり
10 mg $122 在庫あり
25 mg $244 在庫あり
50 mg $366 在庫あり
100 mg $550 在庫あり
200 mg $822 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 43 publication(s) in Google Scholar

Other Forms of Nutlin-3:

Nutlin-3 関連抗体

Top Publications Citing Use of Products

顧客検証

Cell Imaging/Staining
Bio/Physico-chemical Assay
IP
WB
Cell Proliferation/Viability Assay

    Nutlin-3 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Apr 3;15(1):2875.  [Abstract]

    Nutlin-3 (5 μM; 24 h). The interaction between p53 1–50 and MDM2 1-118 was inhibited by Nutlin-3 treatment.

    Nutlin-3 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2022 Sep 2;82(17):3032-3044.  [Abstract]

    Relative luciferase activities of indicated SQLE promoter reporters in C4-2 cells treated with 20 μM LY294002 or 10 μM Nutlin-3 for 12 h.

    Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct;48:248-263.  [Abstract]

    Nutlin-3 (5 μM; 24 h). Binding capacity of MDM2 to p53 in HCT116 cells overexpressing p52-ZER6 and treated with Nutlin-3. Cells are treated with MG132 to inhibit proteasomal degradation. Cell lysates are immunoprecipitated against anti-p53 antibody. The presence ofMDM2 is detected by immunoblotting.

    Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct;48:248-263.  [Abstract]

    Nutlin-3 (5 μM; 24 h). p53 and p21 protein accumulation in HCT116 cells overexpressing p52-ZER6 and treated with Nutlin-3, as examined using western blotting.

    Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct;48:248-263.  [Abstract]

    Nutlin-3 (5 μM; 24 h). Proliferation of p52-ZER6-overexpressed HCT116 cells treated with nutlin-3, as determined by the EdU incorporation assay. Representative images were shown.

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

    IC50 & Target

    Ki: 90 nM (p53-MDM2)[1]
    体外実験

    Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines[3].

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

    Nutlin-3 関連抗体
    体内実験

    Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo[3].

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

    581.49

    分子式

    C30H30Cl2N4O4
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NCCN(C(N2[C@@H](C3=CC=C(Cl)C=C3)[C@@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    Ethanol : 100 mg/mL (171.97 mM; Need ultrasonic)

    DMSO : ≥ 50 mg/mL (85.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7197 mL 8.5986 mL 17.1972 mL
    5 mM 0.3439 mL 1.7197 mL 3.4394 mL
    10 mM 0.1720 mL 0.8599 mL 1.7197 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

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

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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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    体内:

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

      Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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% EtOH    90% Corn Oil

      Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  15% Cremophor EL    85% Saline

      Solubility: 15.15 mg/mL (26.05 mM); Clear solution; Need ultrasonic

    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.
    純度とドキュメンテーション

    純度: 99.18%

    COA (266 KB) HNMR (143 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 µg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2]

    Mice[2]
    Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 / Ethanol 1 mM 1.7197 mL 8.5986 mL 17.1972 mL 42.9930 mL
    5 mM 0.3439 mL 1.7197 mL 3.4394 mL 8.5986 mL
    10 mM 0.1720 mL 0.8599 mL 1.7197 mL 4.2993 mL
    15 mM 0.1146 mL 0.5732 mL 1.1465 mL 2.8662 mL
    20 mM 0.0860 mL 0.4299 mL 0.8599 mL 2.1497 mL
    25 mM 0.0688 mL 0.3439 mL 0.6879 mL 1.7197 mL
    30 mM 0.0573 mL 0.2866 mL 0.5732 mL 1.4331 mL
    40 mM 0.0430 mL 0.2150 mL 0.4299 mL 1.0748 mL
    50 mM 0.0344 mL 0.1720 mL 0.3439 mL 0.8599 mL
    60 mM 0.0287 mL 0.1433 mL 0.2866 mL 0.7166 mL
    80 mM 0.0215 mL 0.1075 mL 0.2150 mL 0.5374 mL
    Ethanol 100 mM 0.0172 mL 0.0860 mL 0.1720 mL 0.4299 mL
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    Nutlin-3 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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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.

    Keywords:

    Nutlin-3548472-68-0Nutlin3Nutlin 3MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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