PROTAC MDM2 Degrader-1
Based on 1 Customer Validation
PROTAC MDM2 Degrader-1 (Compound 15a) is a MDM2 PROTAC degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect.
(Pink: MDM2 ligand (HY-128836); Blue: MDM2 ligand (HY-128836); Black: linker (HY-128844)).
For research use only. We do not sell to patients.
- Purity: 98.11%
- CAS No.: 2249944-98-5
- Formula: C74H84Cl4N10O13
- Molecular Weight:1463.33
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
All PROTACs Isoforms
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Biological Activity
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MDM2 |
PROTAC MDM2 Degrader-1 (5-20 μM; 12 h) inhibits MDM2 expression and promotes p53 expression in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:5 and 20 μM
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Incubation Time:12 h
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Result:Reduced the level of MDM2.
Increased the level of p53.
Chemical Information
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CAS No. 2249944-98-5
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Appearance Solid
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Molecular Weight 1463.33
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Formula C74H84Cl4N10O13
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Color White to off-white
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SMILES
O=C(N1CC(N(CC1)CC(NCCCOCCOCCOCCCNC(CN2C(CN(CC2)C(N3[C@@H](C4=CC=C(C=C4)Cl)[C@@H](C5=CC=C(C=C5)Cl)N=C3C6=C(C=C(C=C6)OC)OC(C)C)=O)=O)=O)=O)=O)N7[C@@H](C8=CC=C(C=C8)Cl)[C@@H](C9=CC=C(C=C9)Cl)N=C7C%10=C(C=C(C=C%10)OC)OC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (68.34 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (270 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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Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 0.6834 mL | 3.4169 mL | 6.8337 mL | 17.0843 mL |
| 5 mM | 0.1367 mL | 0.6834 mL | 1.3667 mL | 3.4169 mL | |
| 10 mM | 0.0683 mL | 0.3417 mL | 0.6834 mL | 1.7084 mL | |
| 15 mM | 0.0456 mL | 0.2278 mL | 0.4556 mL | 1.1390 mL | |
| 20 mM | 0.0342 mL | 0.1708 mL | 0.3417 mL | 0.8542 mL | |
| 25 mM | 0.0273 mL | 0.1367 mL | 0.2733 mL | 0.6834 mL | |
| 30 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5695 mL | |
| 40 mM | 0.0171 mL | 0.0854 mL | 0.1708 mL | 0.4271 mL | |
| 50 mM | 0.0137 mL | 0.0683 mL | 0.1367 mL | 0.3417 mL | |
| 60 mM | 0.0114 mL | 0.0569 mL | 0.1139 mL | 0.2847 mL |