1. Apoptosis
  2. MDM-2/p53
  3. Nutlin (3)

Nutlin (3) 

Cat. No.: HY-50696 Purity: 98.32%
Handling Instructions

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

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

Nutlin (3) Chemical Structure

Nutlin (3) Chemical Structure

CAS No. : 548472-68-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 123 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 936 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Nutlin (3):

Top Publications Citing Use of Products

    Nutlin (3) purchased from MCE. Usage Cited in: EBioMedicine. 2019 Sep 11. pii: S2352-3964(19)30592-4.

    Binding capacity of MDM2 to p53 in HCT116 cells overexpressing p52-ZER6 and treated with nutlin-3 (final concentration: 5 μM). 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 MCE. Usage Cited in: EBioMedicine. 2019 Sep 11. pii: S2352-3964(19)30592-4.

    p53 and p21 protein accumulation in HCT116 cells overexpressing p52-ZER6 and treated with nutlin-3 (final concentration: 5 μM), as examined using western blotting.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    Ki: 90 nM (p53-MDM2)[1]

    In Vitro

    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].

    In Vivo

    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].

    Molecular Weight

    581.49

    Formula

    C₃₀H₃₀Cl₂N₄O₄

    CAS No.

    548472-68-0

    SMILES

    O=C(N1C(C2=C(C=C(C=C2)OC)OC(C)C)=N[[email protected]](C3=CC=C(C=C3)Cl)[[email protected]@H]1C4=CC=C(C=C4)Cl)N5CC(NCC5)=O.[relative stereochemistry]

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (85.99 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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].

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

    Animal Administration
    [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.

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

    References

    Purity: 98.32%

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    Nutlin (3)
    Cat. No.:
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