1. Apoptosis
  2. MDM-2/p53

Nutlin 3 

Cat. No.: HY-50696 Purity: 98.32%
Data Sheet SDS 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
10 mM * 1 mL in DMSO $102 In-stock
5 mg $80 In-stock
10 mg $120 In-stock
50 mg $450 In-stock
100 mg $780 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Nutlin 3:

    Nutlin 3 purchased from MCE. Usage Cited in: Oncotarget. 2016 Mar 22;7(12):14458-75.

    Immunoblot analysis of MCF7 cells reveals that addition of GSK2830371 results in a rapid phosphorylation of p53 at Ser15. Two days after addition of GSK2830371, MCF7 cells show increased levels of p21 which indicates a strong activation of the p53 pathway.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [2]

    Nutlin 3 (NUT) is dissolved with DMSO (100 mM) and diluted with appropriate media[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]

    Nutlin 3 is prepared in EtOH: Tween: 5% Glucose=5:5:90 (Mice)[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
    Molecular Weight

    581.49

    Formula

    C₃₀H₃₀Cl₂N₄O₄

    CAS No.

    548472-68-0

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    Nutlin 3
    Cat. No.:
    HY-50696
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