(R)-CDK2 degrader 6
Based on 1 Customer Validation
(R)-CDK2 degrader 6 is the R-enantiomer of CDK2 degrader 6 (HY-176444), a cereblon-based molecular glue degrader of CDK2 with a DC50 of 27 nM. (R)-CDK2 degrader 6 induces ubiquitination and proteasomal degradation of CDK2 by bridging cereblon and CDK2. (R)-CDK2 degrader 6 is applicable for cancer research.
For research use only. We do not sell to patients.
- Purity: 99.55%
- CAS No.: 3083777-50-5
- Formula: C23H22F5N5O3
- Molecular Weight:511.44
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK2 27 nM (DC50) |
(R)-CDK2 degrader 6 (compound 7, 24 h) potently mediates the degradation of CDK2 in CDK2-HiBiT knock-in HEK293 clone cells stably expressing LgBiT protein. After 24 hours of treatment, the CDK2 level is maximally reduced by 62.2%, with a DC50 of 27.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3083777-50-5
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Appearance Solid
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Molecular Weight 511.44
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Formula C23H22F5N5O3
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SMILES
FC(F)(C12CC(C2)(C3=NN=C(N[C@@H]4[C@H](N(C5=CC(F)=C([C@@H]6C(NC(CC6)=O)=O)C(F)=C5)C4)C)O3)C1)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (195.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 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 (stored under nitrogen, 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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.89 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 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.89 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.
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, 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.
Purity & Documentation
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Data Sheet (274 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, 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 | 1.9553 mL | 9.7763 mL | 19.5526 mL | 48.8816 mL |
| 5 mM | 0.3911 mL | 1.9553 mL | 3.9105 mL | 9.7763 mL | |
| 10 mM | 0.1955 mL | 0.9776 mL | 1.9553 mL | 4.8882 mL | |
| 15 mM | 0.1304 mL | 0.6518 mL | 1.3035 mL | 3.2588 mL | |
| 20 mM | 0.0978 mL | 0.4888 mL | 0.9776 mL | 2.4441 mL | |
| 25 mM | 0.0782 mL | 0.3911 mL | 0.7821 mL | 1.9553 mL | |
| 30 mM | 0.0652 mL | 0.3259 mL | 0.6518 mL | 1.6294 mL | |
| 40 mM | 0.0489 mL | 0.2444 mL | 0.4888 mL | 1.2220 mL | |
| 50 mM | 0.0391 mL | 0.1955 mL | 0.3911 mL | 0.9776 mL | |
| 60 mM | 0.0326 mL | 0.1629 mL | 0.3259 mL | 0.8147 mL | |
| 80 mM | 0.0244 mL | 0.1222 mL | 0.2444 mL | 0.6110 mL | |
| 100 mM | 0.0196 mL | 0.0978 mL | 0.1955 mL | 0.4888 mL |
(R)-CDK2 degrader 6 Related Classifications
HY-176444A Related Classifications
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