CDK2/MDM2-IN-1
Based on 1 Customer Validation
CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC50 value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity.
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- Pureté : 98.07%
- CAS No.: 3083904-06-4
- Formule: C26H33N5O4
- Masse moléculaire:479.57
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
CDK2/ MDM2-IN-1 (100, 200 nM, 4 h) inhibits the proliferation of tumor cells through CDK2/p-Rb and MDM2/p53 pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HCT116, OVCAR3
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Concentration:100, 200 nM
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Incubation Time:4 h
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Result:Reduced the expression of p-Rb, downstream of CDK2.
Inhibited MDM2 protein expression and elevated p53 expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A nude mouse model of HCT116 transplanted tumor[1]
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Dosage:25, 50 mg/kg
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Administration:i.p. for 14 days
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Result:Reduced tumor volume and weight.
Chemical Information
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CAS No. 3083904-06-4
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Appearance Solid
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Masse moléculaire 479.57
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Formule C26H33N5O4
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Color White to off-white
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SMILES
[H][C@]1(C2=CC(NC(CC3=CC=C(N4CCCC4=O)C=C3)=O)=NN2)CC[C@@H](OC(N5CCC5(C)C)=O)C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (208.52 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 (protect from light). 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 (protect from light). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
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Fiche technique (272 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 (protect from light). 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 | 2.0852 mL | 10.4260 mL | 20.8520 mL | 52.1300 mL |
| 5 mM | 0.4170 mL | 2.0852 mL | 4.1704 mL | 10.4260 mL | |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0852 mL | 5.2130 mL | |
| 15 mM | 0.1390 mL | 0.6951 mL | 1.3901 mL | 3.4753 mL | |
| 20 mM | 0.1043 mL | 0.5213 mL | 1.0426 mL | 2.6065 mL | |
| 25 mM | 0.0834 mL | 0.4170 mL | 0.8341 mL | 2.0852 mL | |
| 30 mM | 0.0695 mL | 0.3475 mL | 0.6951 mL | 1.7377 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5213 mL | 1.3033 mL | |
| 50 mM | 0.0417 mL | 0.2085 mL | 0.4170 mL | 1.0426 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3475 mL | 0.8688 mL | |
| 80 mM | 0.0261 mL | 0.1303 mL | 0.2607 mL | 0.6516 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2085 mL | 0.5213 mL |
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