MLN8054

Cat. No.: HY-10180 Purity: 99.54%: FAQs
Data Sheet SDS COA 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

CAS No. : 869363-13-3

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 160	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 160	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 251	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 779	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1081	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE MLN8054

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Aurora Kinase Aurora A Aurora B Aurora C

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]

Aurora A

4 nM (IC₅₀)

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].

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

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].

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

Clinical Trial

Molecular Weight

476.86

Appearance

Solid

Formula

C₂₅H₁₅ClF₂N₄O₂

CAS No.

869363-13-3

SMILES

O=C(C1=CC=C(NC2=NC3=C(CN=C(C4=C3C=CC(Cl)=C4)C5=C(F)C=CC=C5F)C=N2)C=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 : 20.83 mg/mL (43.68 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent 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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.24 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (286 KB) SDS (251 KB)

COA (261 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. [Content Brief]

[2]. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. [Content Brief]

Cell Assay ^[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]	Mice: 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	[1]. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. [Content Brief] [2]. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. [Content Brief]

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.

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

MLN8054869363-13-3MLN 8054MLN-8054Aurora KinaseInhibitorinhibitorinhibit

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MLN8054

Customer Review

9 Publications Citing Use of MCE MLN8054

Featured Recommendations

•Related Screening Libraries:

View All Aurora Kinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

Customer Review

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