PROTAC AAK1 degrader-1
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC50 of <10 nM. PROTAC AAK1 degrader-1 does not significantly impact the levels of any other NAK family members, including BMP2K, GAK, and STK16. PROTAC AAK1 degrader-1 can be used in ovarian cancer research.
For research use only. We do not sell to patients.
- CAS No.: 3113123-63-7
- Formula: C48H56F3N7O4
- Molecular Weight:852.00
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All PROTACs Isoforms
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Biological Activity
PROTAC AAK1 Degrader-1 (1-100 nM, 1-24 h)’s effect on AAK1 protein levels is rapid, noticeable within one hour, and lasted for 3-4 days after 4-hour 14 treatment followed by extensive drug wash-off. PROTAC AAK1 Degrader-1 is also effective in reducing AAK1 levels in a panel of ovarian cancer cell lines including Taxane-resistant sublines (A2780- R and HEY-R) as well as various other cancer types[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3113123-63-7
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Appearance Solid
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Molecular Weight 852.00
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Formula C48H56F3N7O4
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Color White to off-white
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SMILES
CC(C[C@@H](COC1=CC=C(C=C1C(F)(F)F)C2=CC(NC3=CC=C(C=C3)C4CCN(CC4)CC5CCN(CC5)C6=CC7=C(C(N(C7)C8CCC(NC8=O)=O)=O)C=C6)=NC=C2)N)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (117.37 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 (2.93 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 (266 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 | 1.1737 mL | 5.8685 mL | 11.7371 mL | 29.3427 mL |
| 5 mM | 0.2347 mL | 1.1737 mL | 2.3474 mL | 5.8685 mL | |
| 10 mM | 0.1174 mL | 0.5869 mL | 1.1737 mL | 2.9343 mL | |
| 15 mM | 0.0782 mL | 0.3912 mL | 0.7825 mL | 1.9562 mL | |
| 20 mM | 0.0587 mL | 0.2934 mL | 0.5869 mL | 1.4671 mL | |
| 25 mM | 0.0469 mL | 0.2347 mL | 0.4695 mL | 1.1737 mL | |
| 30 mM | 0.0391 mL | 0.1956 mL | 0.3912 mL | 0.9781 mL | |
| 40 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7336 mL | |
| 50 mM | 0.0235 mL | 0.1174 mL | 0.2347 mL | 0.5869 mL | |
| 60 mM | 0.0196 mL | 0.0978 mL | 0.1956 mL | 0.4890 mL | |
| 80 mM | 0.0147 mL | 0.0734 mL | 0.1467 mL | 0.3668 mL | |
| 100 mM | 0.0117 mL | 0.0587 mL | 0.1174 mL | 0.2934 mL |