MLN8054

Catalog No.S1100

For research use only.

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.

MLN8054 Chemical Structure

CAS No. 869363-13-3

Selleck's MLN8054 has been cited by 41 publications

Purity & Quality Control

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Biological Activity

Description MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
Targets
Aurora A [1]
(Sf9 cells)
Aurora B [1]
(Sf9 cells)
4 nM 172 nM
In vitro

MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, which shows >40-fold more selective inhibitory activity for Aurora A compared with Aurora B. [1] In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. [1] A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MWHGeY5kfGmxbjDhd5NigQ>? MnvnTY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCDdYLvdoEhSSCtaX7hd4Uh\XiycnXzd4VlKGmwIHnud4VkfCCVZkmgZ4VtdHNiYomgdoFlcW:jY4TpeoUh\myjc3jwcIF1\SCjc4PhfUwhUUN3ME20JI5O NEHuNIsyPzN4MES4OS=>
human HCT116 cells MmDYSpVv[3Srb36gZZN{[Xl? M3f5dmlvcGmkaYTpc44hd2ZiYYXyc5JiKGurbnHz[UBCKGG3dH;wbI9{eGixconsZZRqd25iYYSgWFI5QCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZpkhcW2vdX7v[ox2d3Knc3PlcoNmKGGwYXz5d4l{NCCLQ{WwQVAvODN2IN88US=> MofRNlYyODF3NkS=
human HeLa cells MmrCSpVv[3Srb36gZZN{[Xl? Ml32NUBp Mof3TY5pcWKrdHnvckBw\iCDdYLvdoEhSSCWaIKyPFgh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDFiaIKsJGlEPTB;MD6wN|Qh|ryP M4j6RlE4OzZyNEi1
human H460 cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 NFHxN446PiCq NV36WWdwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDCdoRWKGOnbHygdJJwdGmoZYLheIlwdiCHTFnTRUwhUUN3ME2wMlEyKM7:TR?= NUfNfFh7OTd|NkC0PFU>
human HT-29 cells MlPFVJJwdGmoZYLheIlwdiCjc4PhfS=> M3PaXlQh\GG7cx?= MojkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB2IHThfZMh[nliY3XscJRqfGW{IHHzd4F6NCCLQ{WwQVAvOTVizszN NHrZO3QyQTRyMk[zNy=>
human Calu6 cells MnLiVJJwdGmoZYLheIlwdiCjc4PhfS=> NWX4O4RjQTZiaB?= Mny4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYXz1OkBk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MD6yNkDPxE1? NVzhOZkyOTd|NkC0PFU>
human SKOV3 cells NVrPVGtvWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYG5OkBp MnPQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MD61N{DPxE1? NILGSGUyPzN4MES4OS=>
human MCF7 cells M3G2VHBzd2yrZnXyZZRqd25iYYPzZZk> M4nhTVk3KGh? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEK{ZGWgZ4VtdCCycn;sbYZmemG2aX;uJGVNUVODLDDJR|UxRTBwNkeg{txO M4G3NlE4OzZyNEi1
human MDAMB231 cells NULLcppYWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVS5OkBp MkDyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFHNRlI{OSClZXzsd{Bi\nSncjC5OkBpenNiYomgRpJlXSClZXzsJJBzd2yrZnXyZZRqd25iRVzJV2EtKEmFNUC9NE44PCEQvF2= NGmwU4QyPzN4MES4OS=>
human PC3 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 M4L5eFk3KGh? MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA6PiCqcoOgZpkhSnKmVTDj[YxtKHC{b3zp[oVz[XSrb36gSWxKW0FuIFnDOVA:OC55OTFOwG0> MVmxO|M3ODR6NR?=
human SW480 cells NF60[3NRem:uaX\ldoF1cW:wIHHzd4F6 M3;4bFk3KGh? NGPmXVdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOFgxKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDCdoRWKGOnbHygdJJwdGmoZYLheIlwdiCHTFnTRUwhUUN3ME2wMlg3KM7:TR?= MVexO|M3ODR6NR?=
human DLD1 cells NV;NOnVyWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3jwO|k3KGh? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESOREGgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEK{ZGWgZ4VtdCCycn;sbYZmemG2aX;uJGVNUVODLDDJR|UxRTFwNEOg{txO M36wXlE4OzZyNEi1
DU-145 prostate cancer cell Mn7WSpVv[3Srb36gZZN{[Xl? MVO5OkBp NVG1ZXFIUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgSHUuOTR3IIDyc5N1[XSnIHPhcoNmeiClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkA6PiCqcjygTWM2OD1yLkGxJO69VQ>? MUixOlExPzF3Mh?=
In vivo In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). MLN8054 also shows similar antitumor activity in the PC-3 tumor xenograft in nude mice. [1] In the HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body area, consistent with a senescent phenotype by increasing senescence-associated beta-galactosidase activity. [3]

Protocol (from reference)

Kinase Assay:[1]
  • Enzyme Assays :

    Recombinant murine Aurora A and Aurora B protein are expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5)/10 mM MgCl2/5 mM DTT/0.05% Tween 20/2 μM peptide substrate/3.3 μCi/ml [γ-33P]ATP at 2 μM by using Image FlashPlates. Aurora B kinase (2 nM) is assayed with 10 μM biotinylated peptide Biotin-TKQTARKSTGGKAPR in 50 mM Tricine (pH 8.0)/2.5 mM MgCl2/5 mM DTT/10% glycerol/2% BSA/40 μCi/ml [γ-33P]ATP at 250 μM. The conditions for all other in vitro kinase assays are available upon request. MLN8054 is run in a 226 kinase screen at a 1 μM compound concentration with an ATP concentration of 10 μM for all assays.

Cell Research:[1]
  • Cell lines: HCT-116, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460, SKOV-3 and PC-3 cells
  • Concentrations: 0.04-10 mM
  • Incubation Time: 96 hours
  • Method: Human tumor cell lines are grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, is added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 mM 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) serves as the untreated control. The cells are treated with MLN8054 for 96 hours 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 according to the manufacturer's recommendation
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: HCT-116 and PC-3 cells are injected s.c. into the right flank of nude mice.
  • Dosages: ≤30 mg/kg
  • Administration: Administered via p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 95 mg/mL
(199.21 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.

30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 476.86
Formula

C25H15ClF2N4O2

CAS No. 869363-13-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)C(=N1)C4=C(C=CC=C4F)F)NC5=CC=C(C=C5)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00652158 Terminated Drug: MLN8054 Advanced Malignancies Millennium Pharmaceuticals Inc. April 2006 Phase 1
NCT00249301 Terminated Drug: MLN8054 Breast Neoplasm|Colon Neoplasm|Pancreatic Neoplasm|Bladder Neoplasm Millennium Pharmaceuticals Inc. October 2005 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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