MLN8054

Name: MLN8054
Brand: MedChemExpress
SKU: HY-10180
Rating: 5.0 (10 reviews)

Cat. No.: HY-10180 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of MLN8054:

MLN8054 sodium Get quote

10 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)

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-6	IC₅₀	0.22 μM Compound: MLN-8054	Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
DLD-1	IC₅₀	1.43 μM Compound: MLN-8054	Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
HCT-116	IC₅₀	0.1 μM Compound: 1, MLN-8054	Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay	[PMID: 19402633]
HCT-116	IC₅₀	0.16 μM Compound: 1, MLN-8054	Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	0.18 μM Compound: MLN-8054	Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
HCT-116	GI₅₀	0.22 μM Compound: 8, MLN8054	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay	[PMID: 26101564]
HCT-116	IC₅₀	0.31 μM Compound: 1, MLN-8054	Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	0.69 μM Compound: MLN8054	Cytotoxicity against human HCT116 cells after 5 days by MTS assay Cytotoxicity against human HCT116 cells after 5 days by MTS assay	[PMID: 22326168]
HCT-116	IC₅₀	0.85 μM Compound: MLN8054	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30143423]
HCT-116	IC₅₀	34 nM Compound: 8, MLN8054	Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis	[PMID: 26101564]
HCT-116	IC₅₀	34 nM Compound: 4, MLN-8054	Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method	[PMID: 19320489]
HCT-116	IC₅₀	4 μM Compound: 4, MLN-8054	Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method	[PMID: 19320489]
HCT-116	IC₅₀	5 μM Compound: 1, MLN-8054	Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	5.2 μM Compound: 8, MLN8054	Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis	[PMID: 26101564]
HeLa	IC₅₀	0.034 μM Compound: MLN-8054	Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr	[PMID: 17360485]
HeLa	IC₅₀	5.7 μM Compound: MLN-8054	Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr	[PMID: 17360485]
HT-29	IC₅₀	0.15 μM Compound: 1, MLN-8054	Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay	[PMID: 19402633]
MCF7	IC₅₀	0.67 μM Compound: MLN-8054	Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
MDA-MB-231	IC₅₀	0.74 μM Compound: MLN-8054	Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
NCI-H460	IC₅₀	0.11 μM Compound: MLN-8054	Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
PC-3	IC₅₀	0.79 μM Compound: MLN-8054	Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
Sf9	IC₅₀	0.004 μM Compound: MLN-8054	Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay	[PMID: 17360485]
Sf9	IC₅₀	0.172 μM Compound: MLN-8054	Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay	[PMID: 17360485]
Sf9	IC₅₀	172 nM Compound: MLN8054	Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay	[PMID: 24681066]
Sf9	IC₅₀	172 nM Compound: MLN8054	Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay	[PMID: 22803810]
Sf9	IC₅₀	31 nM Compound: 8, MLN8054	Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP	[PMID: 26101564]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay	[PMID: 30502115]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay	[PMID: 24681066]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay	[PMID: 22803810]
SK-OV-3	IC₅₀	0.53 μM Compound: MLN-8054	Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
SW480	IC₅₀	0.86 μM Compound: MLN-8054	Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]

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].

MedChemExpress (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].

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

Clinical Trial

Molecular Weight

476.86

Formula

C₂₅H₁₅ClF₂N₄O₂

CAS No.

869363-13-3

Appearance

Solid

Color

White to yellow

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	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (43.68 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	2.0971 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

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.24 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.54%

Select Batch:

Data Sheet (286 KB) SDS (252 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0971 mL	10.4853 mL	20.9705 mL	52.4263 mL
	5 mM	0.4194 mL	2.0971 mL	4.1941 mL	10.4853 mL
	10 mM	0.2097 mL	1.0485 mL	2.0971 mL	5.2426 mL
	15 mM	0.1398 mL	0.6990 mL	1.3980 mL	3.4951 mL
	20 mM	0.1049 mL	0.5243 mL	1.0485 mL	2.6213 mL
	25 mM	0.0839 mL	0.4194 mL	0.8388 mL	2.0971 mL
	30 mM	0.0699 mL	0.3495 mL	0.6990 mL	1.7475 mL
	40 mM	0.0524 mL	0.2621 mL	0.5243 mL	1.3107 mL

MLN8054 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:

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

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MLN8054

Customer Review

Other Forms of MLN8054:

MLN8054 Related Antibodies

10 Publications Citing Use of MCE MLN8054

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Aurora Kinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

MLN8054 Related Antibodies

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Complete Stock Solution Preparation Table

MLN8054 Related Classifications

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