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> Nutlin-3 [548472-68-0]

Nutlin-3 [548472-68-0]

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Cat# HY-50696-10mg

Size : 10mg

Brand : MedChemExpress

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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].

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

Nutlin-3 Related Antibodies
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].

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

581.49

Formula

C30H30Cl2N4O4
CAS No.
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
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: 

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
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.

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
Purity & Documentation
References

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Description
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Price Bef. VAT
HY-50696-100mg
Nutlin-3 [548472-68-0]
 100mg 
HY-50696-50mg
Nutlin-3 [548472-68-0]
 50mg