dAurAB5
Based on 1 Customer Validation
dAurAB5 is a potent Aurora-A/Aurora-B PROTAC degrader with DC50 values of 8.8 nM and 6.1 nM, respectively. dAurAB5 promotes proteasomal degradation of target proteins, induces ubiquitination of Aurora-A and Aurora-B kinases, and downregulates the protein levels of TTK and MYCN. dAurAB5 can be used in studies related to neuroblastoma[1].
(Pink: Aurora A and Aurora B ligand (HY-168542); Blue: Cereblon ligand (HY-103597); Black: linker (HY-B0236)).
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- Pureté: 99.03%
- CAS No.: 3115765-45-9
- Formule: C42H49N11O7
- Masse moléculaire:819.91
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Aurora-A 8.8 nM (DC50) |
Aurora-B 6.1 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| IMR-32 | DC50 |
8.8 nM
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Degradation of endogenous AURKA in TP53-WT IMR32 MYCN-amplified neuroblastoma cells assessed by western blot-based protein degradation assay.
Degradation of endogenous AURKA in TP53-WT IMR32 MYCN-amplified neuroblastoma cells assessed by western blot-based protein degradation assay.
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40785977 |
| IMR-32 | DC50 |
6.1 nM
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Degradation of endogenous AURKB in TP53-WT IMR32 MYCN-amplified neuroblastoma cells assessed by western blot-based protein degradation assay.
Degradation of endogenous AURKB in TP53-WT IMR32 MYCN-amplified neuroblastoma cells assessed by western blot-based protein degradation assay.
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40785977 |
In Vitro
dAurAB5 (5 nM-1 μM; 24 h) induces dose-dependent degradation of Aurora-A and Aurora-B in IMR32 cells, with DC50 values of 8.8 nM and 6.1 nM, respectively, while reducing MYCN protein levels[1].
dAurAB5 (200 nM; 6 h) downregulates Aurora-A and multiple other targets including TTK in MYCN-amplified Kelly neuroblastoma cells[1].
dAurAB5 (10 nM-1 μM; 24 h) reduces cell viability in IMR32 cells but exerts no significant 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:MYCN-amplified IMR32 neuroblastoma cells
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Concentration:5, 10, 50, 100, 200, 500, 1000 nM
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Incubation Time:24 h
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Result:Degraded Aurora-A and Aurora-B in a dose-dependent manner, and a characteristic "hook effect" was observed at high concentrations.
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Cell Line:IMR32 and HEK293
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Significantly reduced the viability of IMR32 neuroblastoma cells, but showed no obvious non-specific cytotoxicity in control HEK293 cells.
Chemical Information
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CAS No. 3115765-45-9
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Appearance Solid
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Masse moléculaire 819.91
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
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)
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.
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
dAurAB5 Related Classifications
HY-171770 Related Classifications
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