PROTAC AURKA degrader 2
Based on 1 Customer Validation
PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W008352)).
For research use only. We do not sell to patients.
- Purity: 98.36%
- CAS No.: 3093582-13-6
- Formula: C50H50ClFN8O11
- Molecular Weight:993.43
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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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Aurora A 3.58 nM (IC50) |
Aurora B 77.2 nM (IC50) |
Chemical Information
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CAS No. 3093582-13-6
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Appearance Solid
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Molecular Weight 993.43
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Formula C50H50ClFN8O11
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Color Off-white to yellow
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SMILES
COC1=C(C=CC(NC2=NC=C3CN=C(C4=C(C3=N2)C=CC(Cl)=C4)C5=C(C=CC=C5F)OC)=C1)C(NCCOCCOCCOCCOCCNC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=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 (100.66 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 (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 | 1.0066 mL | 5.0331 mL | 10.0661 mL | 25.1653 mL |
| 5 mM | 0.2013 mL | 1.0066 mL | 2.0132 mL | 5.0331 mL | |
| 10 mM | 0.1007 mL | 0.5033 mL | 1.0066 mL | 2.5165 mL | |
| 15 mM | 0.0671 mL | 0.3355 mL | 0.6711 mL | 1.6777 mL | |
| 20 mM | 0.0503 mL | 0.2517 mL | 0.5033 mL | 1.2583 mL | |
| 25 mM | 0.0403 mL | 0.2013 mL | 0.4026 mL | 1.0066 mL | |
| 30 mM | 0.0336 mL | 0.1678 mL | 0.3355 mL | 0.8388 mL | |
| 40 mM | 0.0252 mL | 0.1258 mL | 0.2517 mL | 0.6291 mL | |
| 50 mM | 0.0201 mL | 0.1007 mL | 0.2013 mL | 0.5033 mL | |
| 60 mM | 0.0168 mL | 0.0839 mL | 0.1678 mL | 0.4194 mL | |
| 80 mM | 0.0126 mL | 0.0629 mL | 0.1258 mL | 0.3146 mL | |
| 100 mM | 0.0101 mL | 0.0503 mL | 0.1007 mL | 0.2517 mL |