1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Aurora Kinase Apoptosis
  3. Aurkin A

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.

For research use only. We do not sell to patients.

Aurkin A

Aurkin A Chemical Structure

CAS No. : 1534060-58-6

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10 mM * 1 mL in DMSO
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Description

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[1][2].

In Vitro

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.

In Vivo

Aurkin A (30 mg/kg; 15 times, 4 weeks in total) significantly reduces Alisertib (HY-10971)-induced polyploidy formation in mice subcutaneously implanted with VAL cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice treated VAL cells[2]
Dosage: 30 mg/kg
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
Result: Significantly reduced the proportion of polyploid cells induced by alisertib from 43.6% to 16.1%, compared to the alisertib-only group.
Molecular Weight

346.15

Formula

C16H9BrFNO2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C2C=CC=C(F)C2=NC(C3=CC(Br)=CC=C3)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8889 mL 14.4446 mL 28.8892 mL
5 mM 0.5778 mL 2.8889 mL 5.7778 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Aurkin A
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