SK2187
Based on 1 Customer Validation
SK2187 (JB301) is a selective AURKA PROTAC degrader. SK2187 induces targeted degradation of AURKA by recruiting the CRBN E3 ubiquitin ligase. SK2187 is applicable to research related to neuroblastoma.
(Pink: Aurora A ligand (HY-13252); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W015088)).
For research use only. We do not sell to patients.
- Purity: 95.81%
- CAS No.: 3038446-91-9
- Formula: C45H49ClFN7O11S
- Molecular Weight:950.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Aurora A |
SK2187 (10 nM-1 μM; 24 h) induces dose-dependent degradation of AURKA in NGP neuroblastoma cells, with a Dmax,24 h of approximately 85%[1].
SK2187 (10 nM-10 μM; 48 h) potently inhibits the growth of NGP neuroblastoma cells, with an IC50 of 101.5 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NGP neuroblastoma cells
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Concentration:10 nM, 100 nM, 1 μM
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Incubation Time:24 h
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Result:Induced the degradation of AURKA protein, with a maximal degradation (Dmax,24h) of approximately 85% at 10 nM.
Chemical Information
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CAS No. 3038446-91-9
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Appearance Solid
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Molecular Weight 950.43
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Formula C45H49ClFN7O11S
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Color Light yellow to yellow
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SMILES
O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(OCC(NCCOCCOCCOCCNC([C@@]4(CC[C@H](CC4)OC5=C(C(Cl)=CC=C5)F)CC6=CC=CC(NC7=NC=CS7)=N6)=O)=O)=C3C1=O
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Synonyms
JB301
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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 (105.22 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 (2.63 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 (2.63 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.
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 (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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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 | 1.0522 mL | 5.2608 mL | 10.5216 mL | 26.3039 mL |
| 5 mM | 0.2104 mL | 1.0522 mL | 2.1043 mL | 5.2608 mL | |
| 10 mM | 0.1052 mL | 0.5261 mL | 1.0522 mL | 2.6304 mL | |
| 15 mM | 0.0701 mL | 0.3507 mL | 0.7014 mL | 1.7536 mL | |
| 20 mM | 0.0526 mL | 0.2630 mL | 0.5261 mL | 1.3152 mL | |
| 25 mM | 0.0421 mL | 0.2104 mL | 0.4209 mL | 1.0522 mL | |
| 30 mM | 0.0351 mL | 0.1754 mL | 0.3507 mL | 0.8768 mL | |
| 40 mM | 0.0263 mL | 0.1315 mL | 0.2630 mL | 0.6576 mL | |
| 50 mM | 0.0210 mL | 0.1052 mL | 0.2104 mL | 0.5261 mL | |
| 60 mM | 0.0175 mL | 0.0877 mL | 0.1754 mL | 0.4384 mL | |
| 80 mM | 0.0132 mL | 0.0658 mL | 0.1315 mL | 0.3288 mL | |
| 100 mM | 0.0105 mL | 0.0526 mL | 0.1052 mL | 0.2630 mL |
SK2187 Related Classifications
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