MDMX/MDM2-IN-2

Name: MDMX/MDM2-IN-2
Brand: MedChemExpress
SKU: HY-149250
Rating: 4.5 (0 reviews)

Cat. No.: HY-149250 Purity: 98.55%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with K_is of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity.

For research use only. We do not sell to patients.

MDMX/MDM2-IN-2 Chemical Structure

CAS No. : 3043723-74-3

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Description

IC₅₀ & Target

Ki: 0.23 μM (MDM2) and 2.45 μM (MDMX)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BEAS-2B	IC₅₀	17.96 μM Compound: C16	Cytotoxicity against human BEAS-2B cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against human BEAS-2B cells incubated for 72 hrs by CCK-8 assay	[PMID: 36989812]
HCT-116	IC₅₀	0.68 μM Compound: C16	Antiproliferative activity against human HCT-116 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36989812]
L02	IC₅₀	15.93 μM Compound: C16	Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36989812]
SH-SY5Y	IC₅₀	0.54 μM Compound: C16	Antiproliferative activity against human SH-SY5Y cells overexpressing MDMX assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SH-SY5Y cells overexpressing MDMX assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36989812]
SJSA-1	IC₅₀	0.58 μM Compound: C16	Antiproliferative activity against human SJSA-1 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SJSA-1 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36989812]

In Vitro

MDMX/MDM2-IN-2 demonstrates moderate anti-proliferative activities against HCT116 and SH-SY5Y cells (IC₅₀=0.68 μM and 0.54 μM, respectively). MDMX/MDM2-IN-2 possesses low cytotoxicity on normal human lung epithelial BEAS-2B cells and LO2 liver cells (IC₅₀=17.96 μM and 15.93 μM, respectively)^[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) induces apoptosis of HCT116 and SH-SY5Y cells^[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) arrests the cell cycle in G1 phase^[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) increases the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3^[1].
MDMX/MDM2-IN-2 (0.4-0.8 μM) dramatically inhibits colony formation, migration and invasion of HCT116 and SH-SY5Y cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:	HCT116 and SH-SY5Y cells
Concentration:	0.6, 1.2, 2.4 μM
Incubation Time:	48 h
Result:	The percentages of apoptotic HCT116 and SH-SY5Y cells were 13.63% and 15.69% with 0.6 μM. The percentage of apoptotic cells correspondingly increased to 37.6% and 40.8% with 2.4 μM.

Cell Cycle Analysis^[1]

Cell Line:	HCT116 and SH-SY5Y cells
Concentration:	0.6, 1.2, 2.4 μM
Incubation Time:	48 h
Result:	There was an increase in the percentage of cancer cells at the G1 phase. Meanwhile, the percentage of G2 phase cells was relatively decreased.

Western Blot Analysis^[1]

Cell Line:	HCT116 and SH-SY5Y cells
Concentration:	0.6, 1.2, 2.4 μM
Incubation Time:	48 h
Result:	Increased the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3.

Cell Migration Assay ^[1]

Cell Line:	HCT116 and SH-SY5Y cells
Concentration:	0.4, 0.6, 0.8 μM
Incubation Time:	48 h
Result:	Significantly inhibited the migration and invasion in a dose-dependent manner.

Molecular Weight

576.87

Formula

C₂₈H₂₅Cl₃FN₃O₃

CAS No.

3043723-74-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N(C1=CC=C(C=C1)Cl)C(CCC(N2CCNCC2)=O)=O)C3=CC=C(C=C3Cl)F)C4=CC=C(C=C4)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (173.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7335 mL	8.6675 mL	17.3349 mL
5 mM	0.3467 mL	1.7335 mL	3.4670 mL
10 mM	0.1733 mL	0.8667 mL	1.7335 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.67 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.67 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). 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 DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.55%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (250 KB) HNMR (144 KB) RP-HPLC (163 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Hui-Juan Luo, et al. Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer. Eur J Med Chem. 2023 Apr 5;252:115282. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7335 mL	8.6675 mL	17.3349 mL	43.3373 mL
	5 mM	0.3467 mL	1.7335 mL	3.4670 mL	8.6675 mL
	10 mM	0.1733 mL	0.8667 mL	1.7335 mL	4.3337 mL
	15 mM	0.1156 mL	0.5778 mL	1.1557 mL	2.8892 mL
	20 mM	0.0867 mL	0.4334 mL	0.8667 mL	2.1669 mL
	25 mM	0.0693 mL	0.3467 mL	0.6934 mL	1.7335 mL
	30 mM	0.0578 mL	0.2889 mL	0.5778 mL	1.4446 mL
	40 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0834 mL
	50 mM	0.0347 mL	0.1733 mL	0.3467 mL	0.8667 mL
	60 mM	0.0289 mL	0.1445 mL	0.2889 mL	0.7223 mL
	80 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5417 mL
	100 mM	0.0173 mL	0.0867 mL	0.1733 mL	0.4334 mL

MDMX/MDM2-IN-2 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MDMX/MDM2-IN-23043723-74-3MDM-2/p53Apoptosisp53MDMXmigrationinvasionantitumorG1 phaseInhibitorinhibitorinhibit

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MDMX/MDM2-IN-2

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