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AurkA allosteric-IN-1
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Catalog No. T209475
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor with an IC50 of 6.50 μM, which inhibits both the catalytic and non-catalytic activities of Aurora A. Aurora A is involved in the regulation of bipolar mitotic spindle assembly and the fidelity of chromosome segregation during mitosis. AurkA allosteric-IN-1 interferes with Aurora A by binding to the Y-pocket, thereby preventing its interaction with the activator TPX2.
AurkA allosteric-IN-1
AurkA allosteric-IN-1
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Catalog No. T209475
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor with an IC50 of 6.50 μM, which inhibits both the catalytic and non-catalytic activities of Aurora A. Aurora A is involved in the regulation of bipolar mitotic spindle assembly and the fidelity of chromosome segregation during mitosis. AurkA allosteric-IN-1 interferes with Aurora A by binding to the Y-pocket, thereby preventing its interaction with the activator TPX2.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor with an IC50 of 6.50 μM, which inhibits both the catalytic and non-catalytic activities of Aurora A. Aurora A is involved in the regulation of bipolar mitotic spindle assembly and the fidelity of chromosome segregation during mitosis. AurkA allosteric-IN-1 interferes with Aurora A by binding to the Y-pocket, thereby preventing its interaction with the activator TPX2. |
| Targets&IC50 | Aurora A:6.5 μM |
| In vitro | AurkA allosteric-IN-1 demonstrates varying effects on cell cycle arrest across different cell types, including lung and colorectal cancer cell lines, at a concentration of 100 μM over 48 hours. At 20 μM for the same duration, it downregulates histone H3 phosphorylation in cancer cells. Additionally, AurkA allosteric-IN-1 exhibits significant antiproliferative activity against HeLa cells at concentrations ranging from 25 to 400 μM over 48 hours and shows synergistic effects with PHA-767491, enhancing its antiproliferative efficacy further. |
| Formula | C20H16N2O3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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