2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase Polo-like Kinase (PLK)
  4. Aurora Kinases-IN-3

Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10.

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

Aurora Kinases-IN-3 Chemical Structure

Aurora Kinases-IN-3 Chemical Structure

CAS No. : 2840558-83-8

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Customer Review

Based on 1 publication(s) in Google Scholar

Aurora Kinases-IN-3 Related Antibodies

Top Publications Citing Use of Products

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Aurora Kinase Aurora A Aurora B Aurora C

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10[1].

IC50 & Target

AURKB[1]
In Vitro

Aurora Kinases-IN-3 (Compound 15a) (40 nM; 6 h) disrupts localization of AURKB, MKLP1, and PLK at the spindle midzone to prevent spindle midzone microtubule assembly in RPE-MYCBCL2 cells. Aurora Kinases-IN-3 disrupts the localization of AURKB as early as anaphase, producing downstream consequences that blocked cytokinesis[1].
Aurora Kinases-IN-3 (1-10 μM; 3 days) shows wide spectrum of growth suppression in human cancer cell lines[1].

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

Aurora Kinases-IN-3 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI–H23, A549, HCT116, SW480, MDA-MB-231, HeLa and NCI-87 cells
Concentration: 1, 2.5, 5, or 10 μM
Incubation Time: 3 days
Result: Exhibited the EC50 values of about 10 nM in most cell lines.
In Vivo

Aurora Kinases-IN-3 (Compound 15a) (50 mg/kg; oral; twice a day for 7 days) suppresses the growth of lung tumors in mice[1].

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

Animal Model: Female BALB/c nude mice bearing a xenograft of the human lung cancer cell line NCI–H23[1]
Dosage: 50 mg/kg
Administration: Oral gavage, twice a day for 7 days
Result: Elicited a mitotic arrest and induced cell death by apoptosis. Effectively suppressed the growth of the tumor and reduced the cellularity of tumor tissue.
Animal Model: Female BAL B/c nude mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: After oral delivery in PEG300, achieved adequate plasma exposure, the mean value of dose-normalized area under the dose-response curve (AUC) was 0.35 x h/(mg/kg), Cmax was 6.9 μM. Was barely absorbed after oral gavage in the hydrophilic hydroxypropyl methylcellulose (HPMC) formulation.
Molecular Weight

419.35

Formula

C20H16F3N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNC(C1=CC(OC(F)(F)F)=CC(OC2=C(C=CC=N2)C3=CC(OC)=NC=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 (238.46 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 2.3846 mL 11.9232 mL 23.8464 mL
5 mM 0.4769 mL 2.3846 mL 4.7693 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 2.3846 mL 11.9232 mL 23.8464 mL 59.6161 mL
5 mM 0.4769 mL 2.3846 mL 4.7693 mL 11.9232 mL
10 mM 0.2385 mL 1.1923 mL 2.3846 mL 5.9616 mL
15 mM 0.1590 mL 0.7949 mL 1.5898 mL 3.9744 mL
20 mM 0.1192 mL 0.5962 mL 1.1923 mL 2.9808 mL
25 mM 0.0954 mL 0.4769 mL 0.9539 mL 2.3846 mL
30 mM 0.0795 mL 0.3974 mL 0.7949 mL 1.9872 mL
40 mM 0.0596 mL 0.2981 mL 0.5962 mL 1.4904 mL
50 mM 0.0477 mL 0.2385 mL 0.4769 mL 1.1923 mL
60 mM 0.0397 mL 0.1987 mL 0.3974 mL 0.9936 mL
80 mM 0.0298 mL 0.1490 mL 0.2981 mL 0.7452 mL
100 mM 0.0238 mL 0.1192 mL 0.2385 mL 0.5962 mL
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Aurora Kinases-IN-3 Related Classifications

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.

Keywords:

Aurora Kinases-IN-32840558-83-8Aurora KinasePolo-like Kinase (PLK)mitotic localizationMKLP1PLKspindle midzoneNCI–H23A549HCT116SW480MDA-MB-231HeLaNCI-87cancerInhibitorinhibitorinhibit

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