PROTAC DYRK2 degrader-2
Based on 1 Customer Validation
PROTAC DYRK2 degrader-2 is a PROTAC DYRK2 degrader based on curcumin analog A3. It recruits the CRBN E3 ligase to mediate DYRK2 ubiquitination and achieves degradation via the ubiquitin-proteasome system. PROTAC DYRK2 degrader-2 downregulates the expression level of DYRK2 protein in cancer cells. It is applicable to cancer-related research.
(Pink: DYRK2 ligand (HY-186288); Blue: Cereblon ligand (HY-41547); Black: linker (HY-42776)).
For research use only. We do not sell to patients.
- Purity : 98.29%
- CAS No.: 3061366-74-0
- Formula: C42H43Cl2N5O9
- Molecular Weight:832.72
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
DYRK2 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa human cervical carcinoma cells
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Reduced the DYRK2 protein abundance in HeLa cervical cancer cells.
Chemical Information
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CAS No. 3061366-74-0
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Appearance Solid
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Molecular Weight 832.72
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Formula C42H43Cl2N5O9
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Color Light yellow to yellow
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SMILES
O=C1C2=C(NCCOCCOCCOCCNC(CN3C/C(C(/C(C3)=C/C4=C(C=CC=C4)Cl)=O)=C\C5=C(C=CC=C5)Cl)=O)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (60.04 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: ≥ 2.5 mg/mL (3.00 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.
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.
Purity & Documentation
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Data Sheet (273 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. 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 |
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| DMSO | 1 mM | 1.2009 mL | 6.0044 mL | 12.0088 mL | 30.0221 mL |
| 5 mM | 0.2402 mL | 1.2009 mL | 2.4018 mL | 6.0044 mL | |
| 10 mM | 0.1201 mL | 0.6004 mL | 1.2009 mL | 3.0022 mL | |
| 15 mM | 0.0801 mL | 0.4003 mL | 0.8006 mL | 2.0015 mL | |
| 20 mM | 0.0600 mL | 0.3002 mL | 0.6004 mL | 1.5011 mL | |
| 25 mM | 0.0480 mL | 0.2402 mL | 0.4804 mL | 1.2009 mL | |
| 30 mM | 0.0400 mL | 0.2001 mL | 0.4003 mL | 1.0007 mL | |
| 40 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7506 mL | |
| 50 mM | 0.0240 mL | 0.1201 mL | 0.2402 mL | 0.6004 mL | |
| 60 mM | 0.0200 mL | 0.1001 mL | 0.2001 mL | 0.5004 mL |
PROTAC DYRK2 degrader-2 Related Classifications
HY-186287 Related Classifications
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