MDMX/MDM2-IN-2
Based on 1 Customer Validation
MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis 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.
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- Pureté : 98.55%
- CAS No.: 3043723-74-3
- Formule: C28H25Cl3FN3O3
- Masse moléculaire:576.87
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
Ki: 0.23 μM (MDM2) and 2.45 μM (MDMX)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BEAS-2B | IC50 |
17.96 μM
Compound: C16
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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
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[PMID: 36989812] |
| HCT-116 | IC50 |
0.68 μM
Compound: C16
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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
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[PMID: 36989812] |
| L02 | IC50 |
15.93 μM
Compound: C16
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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
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[PMID: 36989812] |
| SH-SY5Y | IC50 |
0.54 μM
Compound: C16
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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
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[PMID: 36989812] |
| SJSA-1 | IC50 |
0.58 μM
Compound: C16
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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
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[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.
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Cell Line:HCT116 and SH-SY5Y cells
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Concentration:0.6, 1.2, 2.4 μM
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Incubation Time:48 h
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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.
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Cell Line:HCT116 and SH-SY5Y cells
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Concentration:0.6, 1.2, 2.4 μM
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Incubation Time:48 h
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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.
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Cell Line:HCT116 and SH-SY5Y cells
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Concentration:0.6, 1.2, 2.4 μM
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Incubation Time:48 h
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Result:Increased the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3.
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Cell Line:HCT116 and SH-SY5Y cells
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Concentration:0.4, 0.6, 0.8 μM
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Incubation Time:48 h
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Result:Significantly inhibited the migration and invasion in a dose-dependent manner.
Chemical Information
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CAS No. 3043723-74-3
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Appearance Solid
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Masse moléculaire 576.87
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Formule C28H25Cl3FN3O3
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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.
| 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
HY-149250 Related Classifications
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