Aurkin A
Based on 1 Customer Validation
Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM. Aurkin A can disrupt polyploidy induced by Alisertib (HY-10971) and increase apoptosis of tumor cells. Aurkin A can be used in research on mitosis and cancer.
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- Pureza: 98.0%
- No. CAS: 1534060-58-6
- Fòrmula: C16H9BrFNO2
- Peso molecular:346.15
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
Aurkin A (10-1000 μM; 2 h) mislocalizes Aurka from the mitotic spindle microtubules in HeLa cells (EC50: 85 μM) and reduces T288 autophosphorylation levels (EC50: 135 μM)[1].
Aurkin A (0-200 µM; 3-5 days) can disrupt Alisertib (HY-10971)-induced polyploidy and increase apoptosis in U2932 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice treated VAL cells[2]
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Dosage:30 mg/kg
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Administration:Once a day for five days a week. After two weeks, treatment was then withheld for a week, followed by another five-day-a-week treatment cycle
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Result:Significantly reduced the proportion of polyploid cells induced by alisertib from 43.6% to 16.1%, compared to the alisertib-only group.
Chemical Information
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No. CAS 1534060-58-6
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Appearance Solid
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Peso molecular 346.15
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Fòrmula C16H9BrFNO2
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Color Light yellow to yellow
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SMILES
O=C(C1=C2C=CC=C(F)C2=NC(C3=CC(Br)=CC=C3)=C1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (288.89 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.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Janeček M, et al., Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2. Sci Rep. 2016 Jun 24;6:28528. [Content Brief]
[2]. Conway PJ, et al. Aurkin-A, a TPX2-Aurora A small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma. Neoplasia. 2024 Sep;55:101014. [Content Brief]
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 | 2.8889 mL | 14.4446 mL | 28.8892 mL | 72.2230 mL |
| 5 mM | 0.5778 mL | 2.8889 mL | 5.7778 mL | 14.4446 mL | |
| 10 mM | 0.2889 mL | 1.4445 mL | 2.8889 mL | 7.2223 mL | |
| 15 mM | 0.1926 mL | 0.9630 mL | 1.9259 mL | 4.8149 mL | |
| 20 mM | 0.1444 mL | 0.7222 mL | 1.4445 mL | 3.6112 mL | |
| 25 mM | 0.1156 mL | 0.5778 mL | 1.1556 mL | 2.8889 mL | |
| 30 mM | 0.0963 mL | 0.4815 mL | 0.9630 mL | 2.4074 mL | |
| 40 mM | 0.0722 mL | 0.3611 mL | 0.7222 mL | 1.8056 mL | |
| 50 mM | 0.0578 mL | 0.2889 mL | 0.5778 mL | 1.4445 mL | |
| 60 mM | 0.0481 mL | 0.2407 mL | 0.4815 mL | 1.2037 mL | |
| 80 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9028 mL | |
| 100 mM | 0.0289 mL | 0.1444 mL | 0.2889 mL | 0.7222 mL |
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