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Nutlin-3b MDM2/MDMX antagonist

Name: Nutlin-3b
Brand: Selleck Chemicals
SKU: S8065
Rating: 5 (2 reviews)

Cat.No.S8065

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of this compound as in comparison with opposite (-)-enantiomer Nutlin-3a.

Chemical Structure

Molecular Weight: 581.49

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Quality Control

Batch: S806501 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.88%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.88

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other MDM2/MDMX Inhibitors	Nutlin-3 RG-7112 Nutlin-3a Brigimadlin Idasanutlin (RG7388) SAR405838 NSC 207895 NVP-CGM097 Siremadlin (HDM201) MX69

Chemical Information, Storage & Stability

Molecular Weight	581.49	Formula	C₃₀H₃₀Cl₂N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	675576-97-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(+)-Nutlin-3			Smiles	CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	MDM2 13.6 μM
In vitro	Nutlin-3b is useful as a negative control for non-MDM2-related cellular activities. Nutlin-3a induces the expression of MDM2 and p21 (but not p53) only in cells with wild-type p53. This compound has no effect regardless of the p53 status of the cells. Only the active enantiomer Nutlin-3a shows a potent antiproliferative activity and clear separation of potency between the cells harbouring wild-type p53 and those harbouring mutant p53. The potency of this chemical is much lower in the wild-type p53 cells and nearly identical to the potency of Nutlin-3a against the mutant p53 cells. After 48 hours of exposure to the Nutlin-3a, 45% of the cell population became TUNEL positive, but cells treated with this compound are indistinguishable from the untreated controls.
Kinase Assay	Biacore study
Kinase Assay	Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilised for the immobilisation 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 this compound 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 this chemical is calculated as a percentage of binding in its absence and IC50 is calculated
References	[1] https://pubmed.ncbi.nlm.nih.gov/14704432/

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