PROTAC AURKA degrader 3
Based on 1 Customer Validation
PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC50 values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia.
(Pink: Aurora A ligand (HY-168545); Blue: Cereblon ligand (HY-10984); Black: linker (HY-N0420)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.78%
- 화학식: C41H41N11O8S
- 분자량:847.90
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
Aurora A 2.05 nM (DC50) |
Aurora B 157.85 nM (DC50) |
TTK 43.05 nM (DC50) |
Cereblon |
In Vitro
PROTAC AURKA degrader 3 (Compound 15) (6 h) efficiently and selectively degrades AURKA in MV4-11AURKA-HiBiT cells, with a DC50 of 2.05 nM, and is 77-fold and 21-fold more selective for AURKB and TTK, respectively[1].
PROTAC AURKA degrader 3 (72 h) potently inhibits the proliferation of quiescent MV4-11 acute myeloid leukemia cells, with an EC50 of 39 nM following 72 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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분자량 847.90
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화학식 C41H41N11O8S
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC(N4CCN(C5=CC=C(NC6=NC(NC7=CC=CC=C7S(=O)(C(C)C)=O)=C8N=CNC8=N6)C=C5)CC4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (117.94 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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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. 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 |
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| DMSO | 1 mM | 1.1794 mL | 5.8969 mL | 11.7938 mL | 29.4846 mL |
| 5 mM | 0.2359 mL | 1.1794 mL | 2.3588 mL | 5.8969 mL | |
| 10 mM | 0.1179 mL | 0.5897 mL | 1.1794 mL | 2.9485 mL | |
| 15 mM | 0.0786 mL | 0.3931 mL | 0.7863 mL | 1.9656 mL | |
| 20 mM | 0.0590 mL | 0.2948 mL | 0.5897 mL | 1.4742 mL | |
| 25 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1794 mL | |
| 30 mM | 0.0393 mL | 0.1966 mL | 0.3931 mL | 0.9828 mL | |
| 40 mM | 0.0295 mL | 0.1474 mL | 0.2948 mL | 0.7371 mL | |
| 50 mM | 0.0236 mL | 0.1179 mL | 0.2359 mL | 0.5897 mL | |
| 60 mM | 0.0197 mL | 0.0983 mL | 0.1966 mL | 0.4914 mL | |
| 80 mM | 0.0147 mL | 0.0737 mL | 0.1474 mL | 0.3686 mL | |
| 100 mM | 0.0118 mL | 0.0590 mL | 0.1179 mL | 0.2948 mL |
PROTAC AURKA degrader 3 Related Classifications
HY-168543 Related Classifications
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