PROTAC DYRK2 degrader 1
Based on 1 Customer Validation
PROTAC DYRK2 degrader 1 is a DYRK2 PROTAC degrader with DC50 values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer.
(Pink: DYRK2 ligand (HY-161598); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42776)).
For research use only. We do not sell to patients.
- Purity : 90.63%
- CAS No.: 3061366-76-2
- Formula: C42H43Br2N5O9
- Molecular Weight:921.63
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
Description
IC50 & Target
[1]|
DYRK2 1.607 μM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
9.1 μM
Compound: CP134
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation by CCK-8 assay
|
[PMID: 38746900] |
In Vitro
Chemical Information
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CAS No. 3061366-76-2
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Appearance Solid
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Molecular Weight 921.63
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Formula C42H43Br2N5O9
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Color Light yellow to yellow
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SMILES
O=C(NCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4C/C(C(/C(C4)=C/C5=CC=CC=C5Br)=O)=C\C6=CC=CC=C6Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (108.50 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)
Purity & Documentation
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Data Sheet (269 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0850 mL | 5.4252 mL | 10.8503 mL | 27.1259 mL |
| 5 mM | 0.2170 mL | 1.0850 mL | 2.1701 mL | 5.4252 mL | |
| 10 mM | 0.1085 mL | 0.5425 mL | 1.0850 mL | 2.7126 mL | |
| 15 mM | 0.0723 mL | 0.3617 mL | 0.7234 mL | 1.8084 mL | |
| 20 mM | 0.0543 mL | 0.2713 mL | 0.5425 mL | 1.3563 mL | |
| 25 mM | 0.0434 mL | 0.2170 mL | 0.4340 mL | 1.0850 mL | |
| 30 mM | 0.0362 mL | 0.1808 mL | 0.3617 mL | 0.9042 mL | |
| 40 mM | 0.0271 mL | 0.1356 mL | 0.2713 mL | 0.6781 mL | |
| 50 mM | 0.0217 mL | 0.1085 mL | 0.2170 mL | 0.5425 mL | |
| 60 mM | 0.0181 mL | 0.0904 mL | 0.1808 mL | 0.4521 mL | |
| 80 mM | 0.0136 mL | 0.0678 mL | 0.1356 mL | 0.3391 mL | |
| 100 mM | 0.0109 mL | 0.0543 mL | 0.1085 mL | 0.2713 mL |