MD-222
Based on 1 publication(s) in Google Scholar
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
(Pink: MDM-2/p53 ligand (HY-125858); Blue: Cereblon ligand (HY-138793); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.03%
- CAS 番号: 2136246-72-3
- 分子式: C48H47Cl2FN6O6
- 分子量:893.83
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 MD-222
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生物活性
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MDM2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
>10 nM
Compound: MD-222
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Binding affinity to cereblon in human MDA-MB-231 cells assessed as cell growth inhibition measured after 4 days
Binding affinity to cereblon in human MDA-MB-231 cells assessed as cell growth inhibition measured after 4 days
|
[PMID: 31560543] |
| MDA-MB-231 | IC50 |
>3 μM
Compound: MD-222
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
|
[PMID: 31560543] |
| MDA-MB-231 | IC50 |
>3 μM
Compound: MD-222
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Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
|
[PMID: 31560543] |
| MDA-MB-231 | IC50 |
>3 μM
Compound: MD-222
|
Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
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[PMID: 31560543] |
| MDA-MB-468 | IC50 |
>10 nM
Compound: MD-222
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Binding affinity to cereblon in human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 days
Binding affinity to cereblon in human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 days
|
[PMID: 31560543] |
| MDA-MB-468 | IC50 |
>3 μM
Compound: MD-222
|
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
|
[PMID: 31560543] |
| MDA-MB-468 | IC50 |
>3 μM
Compound: MD-222
|
Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
|
[PMID: 31560543] |
| MDA-MB-468 | IC50 |
>3 μM
Compound: MD-222
|
Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay
|
[PMID: 31560543] |
| RS4-11 | IC50 |
7.9 nM
Compound: MD-222
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Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay
|
[PMID: 31560543] |
MD-222 (1-30 nM; 1-2 hours) treatment shows very effective in reducing the levels of MDM2 protein and increasing the levels of p53 in a time- and dose-dependent manner in RS4;11 and RS4;11/IRMI-2 cells[1].
MD-222 (30-100 nM; 6 hours) is effective in increasing the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA in RS4;11 cells, indicating strong activation of p53[2].
MD-222 (4 days) shows cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM, and has no effect on RS4;11/IRMI-2, MDA-MB-231 and MDA-MB-468 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 and RS4;11/IRMI-2 cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM
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Incubation Time:1 hour, 2 hours
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Result:Reduced the level of MDM2 and increased the level of p53.
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Cell Line:RS4;11 cells
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Concentration:30 nM, 100 nM
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Incubation Time:6 hours
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Result:Increasd the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA.
化学情報
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CAS 番号 2136246-72-3
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性状 Solid
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分子量 893.83
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分子式 C48H47Cl2FN6O6
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Color White to off-white
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SMILES
O=C1[C@]2(C3=CC=C(Cl)C=C3N1)C4(CCCCC4)N[C@H]([C@]2([H])C5=C(C(Cl)=CC=C5)F)C(NC6=CC=C(C=C6)C(NCCCCCC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]2025 Nov 6;16(1):9805. PMID: 41198675
溶剤 & 溶解度
DMSO : 200 mg/mL (223.76 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.59 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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 (sealed storage, away from moisture)
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.
純度とドキュメンテーション
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データシート (275 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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取扱説明書 (2659 KB)
参考文献
[1]. Jiuling Yang, et al. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders. J Med Chem. 2019 Nov 14;62(21):9471-9487. [Content Brief]
[2]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis TargetingChimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable TumorRegression. J Med Chem. 2019 Jan 24;62(2):448-466. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.1188 mL | 5.5939 mL | 11.1878 mL | 27.9695 mL |
| 5 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL | 5.5939 mL | |
| 10 mM | 0.1119 mL | 0.5594 mL | 1.1188 mL | 2.7970 mL | |
| 15 mM | 0.0746 mL | 0.3729 mL | 0.7459 mL | 1.8646 mL | |
| 20 mM | 0.0559 mL | 0.2797 mL | 0.5594 mL | 1.3985 mL | |
| 25 mM | 0.0448 mL | 0.2238 mL | 0.4475 mL | 1.1188 mL | |
| 30 mM | 0.0373 mL | 0.1865 mL | 0.3729 mL | 0.9323 mL | |
| 40 mM | 0.0280 mL | 0.1398 mL | 0.2797 mL | 0.6992 mL | |
| 50 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5594 mL | |
| 60 mM | 0.0186 mL | 0.0932 mL | 0.1865 mL | 0.4662 mL | |
| 80 mM | 0.0140 mL | 0.0699 mL | 0.1398 mL | 0.3496 mL | |
| 100 mM | 0.0112 mL | 0.0559 mL | 0.1119 mL | 0.2797 mL |
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