2. Cell Cycle/DNA Damage Epigenetics Autophagy
  3. Aurora Kinase Autophagy
  4. MK-5108

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.

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

MK-5108 Chemical Structure

MK-5108 Chemical Structure

CAS No. : 1010085-13-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 102 In-stock
Solution
10 mM * 1 mL in DMSO USD 102 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 100 In-stock
10 mg USD 170 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

MK-5108 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.

IC50 & Target[1]

Aurora A

64 pM (IC50)

In Vitro

MK-5108 inhibits Aurora-A activity with an IC50 value of 0.064 nM in an ATP-competitive manner. It shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 also exhibits high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits the growth of 14 cell lines with IC50 values between 0.16 and 6.4 μM[1].

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

MK-5108 Related Antibodies
In Vivo

MK-5108 treatments at 15 and 30 mg/kg results in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 is well tolerated at both doses, with minimal reduction in body weight. MK-5108 also exhibits significant antitumor activity in nude rats bearing SW48 tumors. MK-5108 at 15 and 45 mg/kg causes dose-dependent tumor growth inhibition with a %T/C of 35% and 7% at day 10, and 58% and 32% at day 27, respectively. MK-5108 is well tolerated in nude rats, with no body weight reduction and moderate effect on blood cells[1].

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

461.94

Formula

C22H21ClFN3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C(Cl)=CC=C1)=C1O[C@H](CC2)CC[C@@]2(C(O)=O)CC3=CC=CC(NC4=NC=CS4)=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (27.06 mM; ultrasonic and warming and heat to 60°C; 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 2.1648 mL 10.8239 mL 21.6478 mL
5 mM 0.4330 mL 2.1648 mL 4.3296 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

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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)

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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: ≥ 1.25 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% Methyl cellulose/0.5% Tween-80 in Saline water

    Solubility: 6.67 mg/mL (14.44 mM); Suspended solution; Need ultrasonic

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

Purity: 99.89%

COA (259 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

The Aurora-A assay reaction is conducted in the presence of 20 μM ATP, 25 μM Tetra-Kemptide, 1.0 μCi per well [γ-33P]-ATP, 0.1 ng per well Aurora-A in 50 mmol/L Tris-HCl (pH 7.4), 15 mmol/L Mg(OAc)2, and 0.2 mmol/L EDTA at 30°C for 40 min. To investigate the inhibition mode of MK-5108 for Aurora-A, the IC50 values of MK-5108 are determined in the presence of different concentrations of ATP. Then, the IC50 value is plotted as a function of ATP concentration to analyze the effect of ATP concentration on the IC50 value of MK-5108[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are seeded in 96-well plates then incubated overnight. A medium containing MK-5108, docetaxel, or DMSO control is added and is incubated for 72 h. The cell population densities are then measured by the WST-8 colorimetric assay using a SpectraMax Plus384 plate reader. Concentration response curves are generated to give the decrease in cell population density in MK-5108– and docetaxel-treated samples relative to DMSO-treated control. Growth inhibition IC50 values are determined from those curves[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: After 8 d, MK-5108 is suspended in 0.5% methyl cellulose/0.24% SDS and orally administered twice daily for 14 d. SW48 cells are suspended in 50% Matrigel/50% PBS and s.c. transplanted into the side flank of nude rats. After 7 d, MK-5108 is suspended in 0.5% methyl cellulose/0.24% SDS and orally administered twice daily for 2 d/wk for 3 wk. In a HeLa-luc and ES-2 dual flank xenograft model, HeLa-luc or ES-2 cells are suspended in 50% Matrigel and 50% PBS, and s.c. transplanted into the right or left side flank of nude rats. After 8 d, vehicle (5% ethanol-saline) or 7.5 mg/kg docetaxel is injected i.v. MK-5108 is orally administered twice daily for 2 d 24 h after the docetaxel injection. The volume of each tumor is determined from the tumor diameter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1648 mL 10.8239 mL 21.6478 mL 54.1196 mL
5 mM 0.4330 mL 2.1648 mL 4.3296 mL 10.8239 mL
10 mM 0.2165 mL 1.0824 mL 2.1648 mL 5.4120 mL
15 mM 0.1443 mL 0.7216 mL 1.4432 mL 3.6080 mL
20 mM 0.1082 mL 0.5412 mL 1.0824 mL 2.7060 mL
25 mM 0.0866 mL 0.4330 mL 0.8659 mL 2.1648 mL
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MK-5108 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:

MK-51081010085-13-8VX-689MK5108MK 5108VX689VX 689Aurora KinaseAutophagyInhibitorinhibitorinhibit

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