CCT400028
Based on 1 Customer Validation
CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-W671452); Black: linker).
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- Pureté: 98.03%
- Formule: C47H49ClFN7O7
- Masse moléculaire:878.39
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Cereblon |
Aurora A 71 nM (Kd) |
Aurora B 2100 nM (Kd) |
Aurora C >10 μM (Kd) |
CCT400028 (0.001-10 μM; 0-24 h) shows no hook effect, potently degrades Aurora A in MV4-11 human pediatric leukemia cells, with a DC50 of 29 nM at 6 h and a DCmax of 85%; it also induces potent and sustained (24 h) Aurora A degradation in human pediatric neuroblastoma Kelly cells[1].
The Aurora A degradation activity of CCT400028 (1 μM; 4 h) in human pediatric neuroblastoma Kelly cells can be blocked by proteasome function inhibitors, Cullin ring ligase activity inhibitors, CRBN-binding inhibitors, and Aurora A-binding inhibitors (inhibitors require 2 h of pre-treatment)[1].
CCT400028 (0.01-10 μM; 72 h) inhibits the viability of human pediatric leukemia cells MV4-11, with a GI50 of 310 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kelly human pediatric neuroblastoma cells
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Concentration:0.001-10 μM
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Incubation Time:4 h; 24 h
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Result:Induced robust, sustained Aurora A depletion at both 4 h and 24 h. Reduced Aurora A levels to near-background at concentrations ≥0.1 μM by 4 h, and maintained this depletion at 24 h. Showed no hook effect across the tested concentration range.
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Cell Line:Kelly human pediatric neuroblastoma cells
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Concentration:1 μM (CCT400028; preceded by 2 h pre-incubation with 10 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062), 10 μM CC220 (HY-101291), 0.25-5 μM Alisertib (HY-10971))
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Incubation Time:4 h (CCT400028 co-treatment; 2 h pre-incubation with inhibitors)
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Result:Induced robust, sustained Aurora A depletion at both 4 h and 24 h.
Showed no hook effect across the tested concentration range.
Induced Aurora A degradation that was completely blocked by pretreatment with the proteasome inhibitor MG132 (HY-13259) and the neddylation inhibitor MLN4924 (HY-70062).
Induced Aurora A degradation that was inhibited by pretreatment with the CRBN ligand CC220 (HY-101291) and the Aurora A inhibitor Alisertib (HY-10971).
Chemical Information
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Appearance Solid
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Masse moléculaire 878.39
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Formule C47H49ClFN7O7
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Color Off-white to light yellow
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SMILES
O=C1NC(CCN1C2=CC=C(C=C2)OCCCCCOCCCCCNC(C3=CC=C(C=C3OC)NC4=NC5=C(C=N4)CN=C(C6=C(C=CC=C6OC)F)C7=CC(Cl)=CC=C57)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (113.84 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (2.85 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (274 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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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 (sealed storage, away from moisture). 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 | 1.1384 mL | 5.6922 mL | 11.3845 mL | 28.4612 mL |
| 5 mM | 0.2277 mL | 1.1384 mL | 2.2769 mL | 5.6922 mL | |
| 10 mM | 0.1138 mL | 0.5692 mL | 1.1384 mL | 2.8461 mL | |
| 15 mM | 0.0759 mL | 0.3795 mL | 0.7590 mL | 1.8974 mL | |
| 20 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4231 mL | |
| 25 mM | 0.0455 mL | 0.2277 mL | 0.4554 mL | 1.1384 mL | |
| 30 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
| 40 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7115 mL | |
| 50 mM | 0.0228 mL | 0.1138 mL | 0.2277 mL | 0.5692 mL | |
| 60 mM | 0.0190 mL | 0.0949 mL | 0.1897 mL | 0.4744 mL | |
| 80 mM | 0.0142 mL | 0.0712 mL | 0.1423 mL | 0.3558 mL | |
| 100 mM | 0.0114 mL | 0.0569 mL | 0.1138 mL | 0.2846 mL |
CCT400028 Related Classifications
HY-181311 Related Classifications
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