dAURK-4
Based on 1 Customer Validation
dAURK-4 is a selective AURKA PROTAC degrader. dAURK-4 promotes ubiquitination and degradation of AURKA. dAURK-4 can be used in the research of glioblastoma and multiple myeloma.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W004640)).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2705844-81-9
- Formula: C52H52ClFN8O12
- Molecular Weight:1035.47
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
|
Aurora A |
Cereblon |
dAURK-4 (1 μM; 5 h) potently and selectively degrades AURKA in MOLT-4 T-lymphoblastic leukemia cells, while exhibits weak activity against AURKB[2].
dAURK-4 (125-1000 nM; 4-24 h) induces dose-dependent degradation of AURKA in MM.1S multiple myeloma cells, and achieves nearly complete degradation at concentrations ≥250 nM[2].
dAURK-4 (0.0001-100 μM; 72 h) exhibits better antiproliferative activity than Alisertib (HY-10971) in MM.1S multiple myeloma cells, with stronger potency at low concentrations and more significant inhibitory effects on cell viability at high concentrations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:125-1000 nM (4 h incubation); 125-1000 nM (24 h incubation)
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Incubation Time:4 h; 24 h
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Result:Induced dose-dependent degradation of AURKA at both 4 h and 24 h.
Caused near-complete loss of AURKA protein at concentrations of 250 nM and higher for both incubation times.
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Cell Line:human MM.1S multiple myeloma cells
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Concentration:0.0001-100 μM
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Incubation Time:72 h
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Result:Reduced relative cell viability to ≤0.6 at concentrations of 0.1 μM and above.
Reduced relative viability to ~0.2 at 10 μM.
Exhibited superior antiproliferative activity compared to parental inhibitor alisertib, which only achieved comparable viability reduction at 1 μM and above and reduced viability to ~0.0 at 10 μM.
Chemical Information
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CAS No. 2705844-81-9
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Appearance Solid
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Molecular Weight 1035.47
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Formula C52H52ClFN8O12
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Color Off-white to light yellow
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SMILES
O=C(N(C1C(NC(CC1)=O)=O)C2=O)C3=C2C=CC=C3OCC(NCCCOCCOCCOCCCNC(C4=CC=C(NC5=NC=C6C(C(C=CC(Cl)=C7)=C7C(C8=C(F)C=CC=C8OC)=NC6)=N5)C=C4OC)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (96.57 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 (protect from light, stored under nitrogen). 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, stored under nitrogen). 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 (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 (protect from light, stored under nitrogen). 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 | 0.9657 mL | 4.8287 mL | 9.6575 mL | 24.1436 mL |
| 5 mM | 0.1931 mL | 0.9657 mL | 1.9315 mL | 4.8287 mL | |
| 10 mM | 0.0966 mL | 0.4829 mL | 0.9657 mL | 2.4144 mL | |
| 15 mM | 0.0644 mL | 0.3219 mL | 0.6438 mL | 1.6096 mL | |
| 20 mM | 0.0483 mL | 0.2414 mL | 0.4829 mL | 1.2072 mL | |
| 25 mM | 0.0386 mL | 0.1931 mL | 0.3863 mL | 0.9657 mL | |
| 30 mM | 0.0322 mL | 0.1610 mL | 0.3219 mL | 0.8048 mL | |
| 40 mM | 0.0241 mL | 0.1207 mL | 0.2414 mL | 0.6036 mL | |
| 50 mM | 0.0193 mL | 0.0966 mL | 0.1931 mL | 0.4829 mL | |
| 60 mM | 0.0161 mL | 0.0805 mL | 0.1610 mL | 0.4024 mL | |
| 80 mM | 0.0121 mL | 0.0604 mL | 0.1207 mL | 0.3018 mL |