Select your Country or Region

  • TargetMol | Compound LibraryArgentinaArgentina
  • TargetMol | Compound LibraryAustraliaAustralia
  • TargetMol | Compound LibraryAustriaAustria
  • TargetMol | Compound LibraryBelgiumBelgium
  • TargetMol | Compound LibraryBrazilBrazil
  • TargetMol | Compound LibraryBulgariaBulgaria
  • TargetMol | Compound LibraryCroatiaCroatia
  • TargetMol | Compound LibraryCyprusCyprus
  • TargetMol | Compound LibraryCzechCzech
  • TargetMol | Compound LibraryDenmarkDenmark
  • TargetMol | Compound LibraryEgyptEgypt
  • TargetMol | Compound LibraryEstoniaEstonia
  • TargetMol | Compound LibraryFinlandFinland
  • TargetMol | Compound LibraryFranceFrance
  • TargetMol | Compound LibraryGermanyGermany
  • TargetMol | Compound LibraryGreeceGreece
  • TargetMol | Compound LibraryHong KongHong Kong
  • TargetMol | Compound LibraryHungaryHungary
  • TargetMol | Compound LibraryIcelandIceland
  • TargetMol | Compound LibraryIndiaIndia
  • TargetMol | Compound LibraryIrelandIreland
  • TargetMol | Compound LibraryIsraelIsrael
  • TargetMol | Compound LibraryItalyItaly
  • TargetMol | Compound LibraryJapanJapan
  • TargetMol | Compound LibraryKoreaKorea
  • TargetMol | Compound LibraryLatviaLatvia
  • TargetMol | Compound LibraryLebanonLebanon
  • TargetMol | Compound LibraryMalaysiaMalaysia
  • TargetMol | Compound LibraryMaltaMalta
  • TargetMol | Compound LibraryMoroccoMorocco
  • TargetMol | Compound LibraryNetherlandsNetherlands
  • TargetMol | Compound LibraryNew ZealandNew Zealand
  • TargetMol | Compound LibraryNorwayNorway
  • TargetMol | Compound LibraryPolandPoland
  • TargetMol | Compound LibraryPortugalPortugal
  • TargetMol | Compound LibraryRomaniaRomania
  • TargetMol | Compound LibrarySingaporeSingapore
  • TargetMol | Compound LibrarySlovakiaSlovakia
  • TargetMol | Compound LibrarySloveniaSlovenia
  • TargetMol | Compound LibrarySpainSpain
  • TargetMol | Compound LibrarySwedenSweden
  • TargetMol | Compound LibrarySwitzerlandSwitzerland
  • TargetMol | Compound LibraryTaiwan,ChinaTaiwan,China
  • TargetMol | Compound LibraryThailandThailand
  • TargetMol | Compound LibraryTurkeyTurkey
  • TargetMol | Compound LibraryUnited KingdomUnited Kingdom
  • TargetMol | Compound LibraryUnited StatesUnited States
  • TargetMol | Compound LibraryOther CountriesOther Countries
Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

Nutlin-3

Nutlin-3
Contact us for more batch information
Select Batch
Purity:99.89%
Resource Download

Nutlin-3

Catalog No. T2158Cas No. 548472-68-0
Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$54In Stock
5 mg$81In Stock
10 mg$126In Stock
25 mg$261In Stock
50 mg$481In Stock
100 mg$522In Stock
1 mL x 10 mM (in DMSO)$111In Stock
Bulk & Custom
Add to Cart

Related Compound Libraries of "Nutlin-3"

Product Introduction

Bioactivity
Description
Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity.
Targets&IC50
MDM2-p53:0.09 μM
In vitro
METHODS: 22RV1 (p53 WT), DU145 (p53 Mut) and PC-3 (p53 Null) cells were treated with Nutlin-3 (2-10 µM) for 48 h. Apoptosis was detected by Hoechst 33342 staining.
RESULTS: Nutlin-3 induced a significant increase in apoptosis in 22RV1 cells, whereas apoptosis was not significantly increased in p53-deficient DU145 or PC-3 cells. Nutlin-3 preferentially increased apoptosis in cells expressing WT p53. [1]
METHODS: H460 and HCT116 p53+/+ cells were treated with Nutlin-3 (0-100 µM) and Inauhzin (0-100 µM) for 72 h. Cell viability was measured by WST assay.
RESULTS: Inauhzin and Nutlin-3 showed significant synergistic effects in inhibiting the growth of both tumor cell lines, as the CI values were significantly less than 1 in the effective dose range, especially when lower doses of Nutlin-3 were used. [2]
In vivo
METHODS: To assay antitumor activity in vivo, Nutlin-3 (150 mg/kg, EtOH: Tween: 5% Glucose = 5:5:90; administered orally twice daily for four days and stopped for two days) and Inauhzin (15 mg/kg, intraperitoneally once daily) were administered to SCID mice bearing HCT116 p53+/+ xenografts for 21 days.
RESULTS: Each compound alone reduced mean tumor volume by less than 20% after 21 days of treatment. However, when both treatments were combined at the same dose, the final average tumor volume was reduced by 60%. inauhzin and Nutlin-3 activated p53 and inhibited the growth of xenograft tumors in the animals. [2]
Kinase Assay
Biacore study: Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25°C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculated
Cell Research
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].
AliasNutlin3
Chemical Properties
Molecular Weight581.49
FormulaC30H30Cl2N4O4
Cas No.548472-68-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (94.58 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7197 mL8.5986 mL17.1972 mL85.9860 mL
5 mM0.3439 mL1.7197 mL3.4394 mL17.1972 mL
10 mM0.1720 mL0.8599 mL1.7197 mL8.5986 mL
20 mM0.0860 mL0.4299 mL0.8599 mL4.2993 mL
50 mM0.0344 mL0.1720 mL0.3439 mL1.7197 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy Nutlin-3 | purchase Nutlin-3 | Nutlin-3 cost | order Nutlin-3 | Nutlin-3 chemical structure | Nutlin-3 in vivo | Nutlin-3 in vitro | Nutlin-3 formula | Nutlin-3 molecular weight