1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

MK-5108 (Synonyms: VX-689)

Cat. No.: HY-13252 Purity: >98.0%
Data Sheet SDS Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
5 mg USD 144 In-stock
10 mg USD 204 In-stock
50 mg USD 540 In-stock
100 mg USD 900 In-stock
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500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 0.064 nM (Aurora-A kinase)[1]

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].

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].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.2165 mL 1.0824 mL 2.1648 mL
Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

461.94

Formula

C₂₂H₂₁ClFN₃O₃S

CAS No.

1010085-13-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 6.4 mg/mL (Need warming)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
MK-5108
Cat. No.:
HY-13252
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