WH-10417-099
Based on 1 Customer Validation
WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
(Pink: PI3Kγ ligand (HY-168319); Blue: Cereblon ligand (HY-41547); Black: linker (HY-115384)).
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- Reinheit: 98.14%
- CAS. Nr.: 2769753-42-4
- Formel: C52H62N8O13S
- Molecular Weight:1039.16
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Cereblon |
CK1 |
WH-10417-099 (1 μM; 1 hour) induces significant bio-ubiquitylation of 8 kinases (STK4, STK35, GSPT1, RIPK2, MAP4K4, STK3, CSNK1D, CSNK1A1) and 1 non-kinase (CSNK1E) in 293TCRBN−/− cells expressing CRBN-BirA and A3-ubiquitin, with only CSNK1E undergoing significant degradation[1].
WH-10417-099 (100 nM; 24 h) treatment of HEK293T cells drives significant downregulation of 14 proteins, including nine kinases, and co-treatment with 10 µM SB-405483 refines this subset of downregulated proteins to a stringent group of shared targets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2769753-42-4
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Appearance Solid
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Molecular Weight 1039.16
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Formel C52H62N8O13S
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Color Light yellow to yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOCCOCCOCCOCCC(NCCCN(C4CC4)S(C5=CC=C(C6=CN=C(N)C(C7=CC(CCNC8=O)=C8C=C7)=C6)C=C5)(=O)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 40 mg/mL (38.49 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 0.9623 mL | 4.8116 mL | 9.6232 mL | 24.0579 mL |
| 5 mM | 0.1925 mL | 0.9623 mL | 1.9246 mL | 4.8116 mL | |
| 10 mM | 0.0962 mL | 0.4812 mL | 0.9623 mL | 2.4058 mL | |
| 15 mM | 0.0642 mL | 0.3208 mL | 0.6415 mL | 1.6039 mL | |
| 20 mM | 0.0481 mL | 0.2406 mL | 0.4812 mL | 1.2029 mL | |
| 25 mM | 0.0385 mL | 0.1925 mL | 0.3849 mL | 0.9623 mL | |
| 30 mM | 0.0321 mL | 0.1604 mL | 0.3208 mL | 0.8019 mL |