dAURK-4 hydrochloride
Based on 1 Customer Validation
dAURK-4 hydrochloride is a selective AURKA PROTAC degrader. dAURK-4 hydrochloride promotes ubiquitination and degradation of AURKA. dAURK-4 hydrochloride can be used in the research of glioblastoma and multiple myeloma.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W004640)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.57%
- Formel: C52H53Cl2FN8O12
- Molecular Weight:1071.93
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Speicherung:
-20°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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Aurora A |
Cereblon |
In Vitro
dAURK-4 (1 μM; 5 h) hydrochloride potently and selectively degrades AURKA in MOLT-4 T-lymphoblastic leukemia cells, while exhibits weak activity against AURKB[2].
dAURK-4 (125-1000 nM; 4-24 h) hydrochloride induces dose-dependent degradation of AURKA in MM.1S multiple myeloma cells, and achieves nearly complete degradation at concentrations ≥250 nM[2].
dAURK-4 (0.0001-100 μM; 72 h) hydrochloride exhibits better antiproliferative activity than Alisertib (HY-10971) in MM.1S multiple myeloma cells, with stronger potency at low concentrations and more significant inhibitory effects on cell viability at high concentrations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:MM.1S multiple myeloma cells
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Concentration:125-1000 nM (4 h incubation); 125-1000 nM (24 h incubation)
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Incubation Time:4 h; 24 h
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Result:Induced dose-dependent degradation of AURKA at both 4 h and 24 h.
Caused near-complete loss of AURKA protein at concentrations of 250 nM and higher for both incubation times.
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Cell Line:human MM.1S multiple myeloma cells
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Concentration:0.0001-100 μM
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Incubation Time:72 h
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Result:Reduced relative cell viability to ≤0.6 at concentrations of 0.1 μM and above.
Reduced relative viability to ~0.2 at 10 μM.
Exhibited superior antiproliferative activity compared to parental inhibitor alisertib, which only achieved comparable viability reduction at 1 μM and above and reduced viability to ~0.0 at 10 μM.
Chemical Information
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Appearance Solid
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Molecular Weight 1071.93
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Formel C52H53Cl2FN8O12
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Color Light yellow to yellow
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SMILES
O=C(N(C1C(NC(CC1)=O)=O)C2=O)C3=C2C=CC=C3OCC(NCCCOCCOCCOCCCNC(C4=CC=C(NC5=NC=C6C(C(C=CC(Cl)=C7)=C7C(C8=C(F)C=CC=C8OC)=NC6)=N5)C=C4OC)=O)=O.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 66.67 mg/mL (62.20 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 5 mg/mL (4.66 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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. * 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.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
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 | 0.9329 mL | 4.6645 mL | 9.3290 mL | 23.3224 mL |
| 5 mM | 0.1866 mL | 0.9329 mL | 1.8658 mL | 4.6645 mL | |
| 10 mM | 0.0933 mL | 0.4664 mL | 0.9329 mL | 2.3322 mL | |
| 15 mM | 0.0622 mL | 0.3110 mL | 0.6219 mL | 1.5548 mL | |
| 20 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1661 mL | |
| 25 mM | 0.0373 mL | 0.1866 mL | 0.3732 mL | 0.9329 mL | |
| 30 mM | 0.0311 mL | 0.1555 mL | 0.3110 mL | 0.7774 mL | |
| 40 mM | 0.0233 mL | 0.1166 mL | 0.2332 mL | 0.5831 mL | |
| 50 mM | 0.0187 mL | 0.0933 mL | 0.1866 mL | 0.4664 mL | |
| 60 mM | 0.0155 mL | 0.0777 mL | 0.1555 mL | 0.3887 mL |
dAURK-4 hydrochloride Related Classifications
HY-137344A Related Classifications
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