dAurAB5
Based on 1 Customer Validation
dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).
(Pink: Aurora A and Aurora B ligand (HY-168542); Blue: Cereblon ligand (HY-103597); Black: linker (HY-B0236)).
For research use only. We do not sell to patients.
- Purity: 99.03%
- CAS No.: 3115765-45-9
- Formula: C42H49N11O7
- Molecular Weight:819.91
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cereblon |
Aurora-A 8.8 nM (DC50) |
Aurora-B 6.1 nM (DC50) |
dAurAB5 (500 nM, 24 h) induces significant degradation of Aurora-A and Aurora-B, with degradation rates of 84% and 82%[1].
dAurAB5 (500 nM, 24 h) reduces N-Myc levels by 45% in IMR32 cells[1].
dAurAB5 (100 nM, 4 h) degrades 83% of Aurora-A and 95% of Aurora-B in IMR32 cells[1].
dAurAB5 (200 nM, 6 h) decreases the abundance Aurora-A and the levels of AAK1, PTK2, GAK, TTK, but does not downregulated Aurora-B abundance in the MYCN-amplified Kelly neuroblastoma cells[1].
dAurAB5 (0-1000 nM, 24 h) reduces cell viability in IMR32 cells, but has minimal cytotoxicity in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IMR32 cells
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Concentration:500 nM
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Incubation Time:24 h
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Result:Reduced N-Myc levels by 45%.
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Cell Line:IMR32 cells
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Concentration:100 nM
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Incubation Time:4 h
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Result:Degraded 83% of Aurora-A and 95% of Aurora-B.
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Cell Line:IMR32 cells
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Concentration:0, 10, 100, 1000 nM
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Incubation Time:24 h
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Result:Significant reduced cell viability, with 45% reduction in cell viability at 100 nM and 55% reduction in cell viability at 1 μM.
Chemical Information
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CAS No. 3115765-45-9
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Appearance Solid
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Molecular Weight 819.91
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Formula C42H49N11O7
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Color Yellow to orange
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SMILES
O=C(NCCCCCC(N1CCN(C2=CC=C(NC3=NC(NC4CCCCC4)=C5N=CNC5=N3)C=C2)CC1)=O)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=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
DMSO : 100 mg/mL (121.96 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)
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.
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 (271 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)
- Portuguese - PT (251 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 | 1.2196 mL | 6.0982 mL | 12.1965 mL | 30.4912 mL |
| 5 mM | 0.2439 mL | 1.2196 mL | 2.4393 mL | 6.0982 mL | |
| 10 mM | 0.1220 mL | 0.6098 mL | 1.2196 mL | 3.0491 mL | |
| 15 mM | 0.0813 mL | 0.4065 mL | 0.8131 mL | 2.0327 mL | |
| 20 mM | 0.0610 mL | 0.3049 mL | 0.6098 mL | 1.5246 mL | |
| 25 mM | 0.0488 mL | 0.2439 mL | 0.4879 mL | 1.2196 mL | |
| 30 mM | 0.0407 mL | 0.2033 mL | 0.4065 mL | 1.0164 mL | |
| 40 mM | 0.0305 mL | 0.1525 mL | 0.3049 mL | 0.7623 mL | |
| 50 mM | 0.0244 mL | 0.1220 mL | 0.2439 mL | 0.6098 mL | |
| 60 mM | 0.0203 mL | 0.1016 mL | 0.2033 mL | 0.5082 mL | |
| 80 mM | 0.0152 mL | 0.0762 mL | 0.1525 mL | 0.3811 mL | |
| 100 mM | 0.0122 mL | 0.0610 mL | 0.1220 mL | 0.3049 mL |