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

MLN8054 

Cat. No.: HY-10180 Purity: >98.0%
Data Sheet SDS Handling Instructions

MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.

For research use only. We do not sell to patients.
MLN8054 Chemical Structure

MLN8054 Chemical Structure

CAS No. : 869363-13-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $190 In-stock
50 mg $590 In-stock
100 mg $819 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.

IC50 & Target

IC50: 4 nM (Aurora A), 172 nM (Aurora B)[1]

In Vitro

MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase. MLN8054 is >40-fold more selective for Aurora A compared with the family member Aurora B. MLN8054 selectively inhibits Aurora A over Aurora B in cultured human tumor cells. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines. MLN8054 effectively inhibits the growth of cells from diverse tissue origins with IC50 values ranging from 0.11 to 1.43 μM[1]. Treatment of human tumor cells grown in culture with MLN8054 shows a number of morphologic and biochemical changes associated with senescence[2].

In Vivo

In the HCT-116 tumor-bearing mice, MLN8054 treatment inhibits tumor growth dose dependently. MLN8054 is generally well tolerated. MLN8054 also inhibits the growth of the PC-3 tumor xenograft in nude mice. MLN8054 Treatment Results in Inhibition of Aurora A, Accumulation of Mitotic Cells, and Apoptosis in vivo[1]. MLN8054 selectively inhibits Aurora A kinase activity when dosed at 30 mg/kg. At this dose in HCT116 tumor tissue, MLN8054 has been shown to inhibit Aurora A autophosphorylation, and induce an increase in the Aurora B substrate, pHisH3[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0971 mL 10.4853 mL 20.9705 mL
5 mM 0.4194 mL 2.0971 mL 4.1941 mL
10 mM 0.2097 mL 1.0485 mL 2.0971 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

MLN8054 is diluted in DMSO[1].

MLN8054 is added to human tumor cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n=6 wells per plate; 0.2% final concentration) served as the untreated control. The cells are treated with MLN8054 for 96 h at 37°C in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

MLN8054 is prepared in 10% hydroxypropyl-β-cyclodextrin with 5% sodium bicarbonate[1].

Mouse: Nude mice bearing HCT-116 tumors are treated orally once per day for 21 consecutive days with either vehicle control or MLN8054 at doses of 3, 10, or 30 mg/kg. Tumor volumes are measured by using a vernier caliper and calculated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

476.86

Formula

C₂₅H₁₅ClF₂N₄O₂

CAS No.

869363-13-3

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: ≥30 mg/mL (Need ultrasonic and warming)

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

Purity: >98.0%

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Product Name:
MLN8054
Cat. No.:
HY-10180
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