Name: MX69
Brand: Selleck Chemicals
SKU: S8403
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: S840301 DMSO]95 mg/mL]false]Ethanol]41 mg/mL]false]Water]Insoluble]false Purity: 99.99%

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

99.99

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) Nutlin-3b

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (200.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 41 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.75mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.675mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	474.57	Formula	C₂₇H₂₆N₂O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1005264-47-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=C(C=C1)NS(=O)(=O)C2=CC3=C(C=C2)NC(C4C3C=CC4)C5=CC=C(C=C5)C(=O)O)C

Mechanism of Action

Targets/IC₅₀/Ki	MDM2 (Cell-free assay) 2.34 μM(Kd)
In vitro	MX69 inhibits expression of both MDM2 and XIAP in a time- and dose-dependent manner. This compound induces ubiquitination of endogenous MDM2 in cancer cells. Downregulation of MDM2 by this chemical is through induction of MDM2 self-ubiquitination and degradation. Half-life of MDM2 in control-treated EU-1 cells is greater than 90 min, whereas this compound treatment decreases the MDM2 half-life to <30 min. In SK-N-SH cells with stably transfected either wild-type (WT)-MDM2 or mutant MDM2-C464A, Treatment with this compound significantly inhibits expression and increased the turnover of WT-MDM2 but not MDM2-C464A. This compound significantly enhances the p53 half-life in WT-MDM2 but not mutant MDM2-C464A-transfected SK-N-SH cells. p53 is stabilized and accumulates in this compound-treated cells. This compound-mediated inhibition of XIAP is MDM2 dependent. Treatment of this chemical activates caspases 3, 7, and 9 as well as the cleavage of the death substrate PARP. This compound also exhibits a significant cytotoxic effect on both ALL and NB lines(cancer cell lines), particularly those lines with MDM2 overexpression and a WTp53 phenotype. This compound-induced cell death is indeed due to apoptosis. This compound-induced cell apoptosis and death are dependent on MDM2, p53, and XIAP expression. This compound shows minimal inhibitory effect on normal human bone marrow in vitro.
In vivo	MX69 has significant apoptotic and anti-proliferative effects on MDM2-expressing cancer cells in vivo. This compound is well tolerated in animals due to the fact that normal cells/tissues express little or no MDM2. No evidence of toxicity after treatment with this chemical at the 100 mg/kg dose. This MDM2-specific agent should not activate either on-target (e.g., p53 induction) or off-target signaling pathways in normal cells. Thus, specific MDM2 inhibitors such as this compound may be excellent candidates for targeted therapy of refractory cancers expressing high levels of MDM2.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27666947/

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MX69 MDM2/MDMX inhibitor

Chemical Structure

Molecular Weight: 474.57