Catalog No.S1100

MLN8054 Chemical Structure

Molecular Weight(MW): 476.86

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.

Size Price Stock Quantity  
In DMSO USD 238 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Cited by 13 Publications

3 Customer Reviews

  • Aurora A and Aurora B activities do not influence the timing of CENP-A assembly. (A) A nascent pool of CENP-A-SNAP was pulse labeled in randomly cycling HeLa cells during which either Aurora A or Aurora B activity was inhibited by treatment with 1µM of MLN8054 or 2µM of ZM447439, respectively. Cells were fixed and counterstained for cyclin B1, CENP-T and with DAPI to indicate G2 status, centromeres and DNA, respectively. Effective kinase inhibition was evident from chromosome segregation defects in mitosis after Aurora A inhibition [indicated by an asterisk and (Hoar et al., 2007)] prior to subsequent CENP-A assembly in G1 or after Aurora B inhibition resulting in cytokinesis failure and multinucleated cells [asterisk and (Ditchfield et al., 2003)]. Representative images of cells in G1 (low cyclin B) and G2 phase (high cyclin B) are shown. (B) Experiment as in A except  that  cells  were  treated  for  one  hour  with  either  Roscovitine  alone  or  in  combination  with  MLN8054  or ZM447439 prior to fixation. Percentage of cells assembling CENP-A-SNAP is indicated [either percent of total cells (in top panel, G1 phase) or percent of cyclin B1 positive cells (bottom panel, G2 phase)]. 

    Dev Cell 2012 22, 52-63. MLN8054 purchased from Selleck.

    Stacked column graphic representing  the effect of the small molecule MLN8054 throughout oocyte developmental progress, namely during metaphase I, telophase I and metaphase II oocytes in different conditions.

    2013 Professora Dra.maria Gabriela Rodrigues(DBA/FCUL). MLN8054 purchased from Selleck.

  • Western blot analysis of p-Aurora A and Aurora A. 0-10μM MLN8054 was added.



    2011 Dr. Zhang of Tianjin Medical University. MLN8054 purchased from Selleck.

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.
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 NFzFS2pHfW6ldHnvckBie3OjeR?= M12xWmlvcGmkaYTpc44hd2ZibX;1d4UhemWlb33ibY5idnRiQYXyc5JiKEFia3nuZZNmKGW6cILld5Nm\CCrbjDpcpNm[3RiU3[5JINmdGy|IHL5JJJi\GmxYXP0bZZmKG[uYYPodIxifGViYYPzZZktKEmFNUC9OEBvVQ>? MX[xO|M3ODR6NR?=
human HCT116 cells M2fYSmZ2dmO2aX;uJIF{e2G7 M3XOemlvcGmkaYTpc44hd2ZiYYXyc5JiKGurbnHz[UBCKGG3dH;wbI9{eGixconsZZRqd25iYYSgWFI5QCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZpkhcW2vdX7v[ox2d3Knc3PlcoNmKGGwYXz5d4l{NCCLQ{WwQVAvODN2IN88US=> NWjTcFlpOjZzMEG1OlQ>
human HeLa cells MVvGeY5kfGmxbjDhd5NigQ>? NHvMVYgyKGh? NGe0WWxKdmirYnn0bY9vKG:oIFH1do9z[SCDIGTodlI5QCCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiMTDodkwhUUN3ME2wMlA{PCEQvF2= NYfCPJVXOTd|NkC0PFU>
human H460 cells NEHDWJZRem:uaX\ldoF1cW:wIHHzd4F6 NICwOpE6PiCq M{HmR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSES2NEBk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MD6xNUDPxE1? NIq1dW8yPzN4MES4OS=>
human HT-29 cells MoT5VJJwdGmoZYLheIlwdiCjc4PhfS=> MkP6OEBl[Xm| MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDRiZHH5d{BjgSClZXzseIl1\XJiYYPzZZktKEmFNUC9NE4yPSEQvF2= M3HQcFE6PDB{NkOz
human Calu6 cells MlvQVJJwdGmoZYLheIlwdiCjc4PhfS=> MoX5PVYhcA>? MkDhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYXz1OkBk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MD6yNkDPxE1? NF\rO24yPzN4MES4OS=>
human SKOV3 cells NX\U[ZdsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWe5OkBp MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCEcnTVJINmdGxicILvcIln\XKjdHnvckBGVEmVQTygTWM2OD1yLkWzJO69VQ>? MVGxO|M3ODR6NR?=
human MCF7 cells NFfadnNRem:uaX\ldoF1cW:wIHHzd4F6 MYG5OkBp NHXlXI1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFLy[HUh[2WubDDwdo9tcW[ncnH0bY9vKEWOSWPBMEBKSzVyPUCuOlch|ryP M{LJUFE4OzZyNEi1
human MDAMB231 cells NIfnNW5Rem:uaX\ldoF1cW:wIHHzd4F6 NWjBfmZuQTZiaB?= M1jFUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBUWIzOzFiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGJz\FViY3XscEBxem:uaX\ldoF1cW:wIFXMTXNCNCCLQ{WwQVAvPzRizszN M4qxblE4OzZyNEi1
human PC3 cells M4fSSnBzd2yrZnXyZZRqd25iYYPzZZk> MUG5OkBp NVfWSI5ySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFLy[HUh[2WubDDwdo9tcW[ncnH0bY9vKEWOSWPBMEBKSzVyPUCuO|kh|ryP M{\M[|E4OzZyNEi1
human SW480 cells NW\S[HlLWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mm\CPVYhcA>? MlfXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{S4NEBk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MD64OkDPxE1? M1fi[FE4OzZyNEi1
human DLD1 cells NHrITmFRem:uaX\ldoF1cW:wIHHzd4F6 MVK5OkBp M4DmOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRFzENUBk\WyuczDh[pRmeiB7NjDodpMh[nliQoLkWUBk\WyuIIDyc4xq\mW{YYTpc44hTUyLU1GsJGlEPTB;MT60N{DPxE1? MmfxNVc{PjB2OEW=
DU-145 prostate cancer cell NWfnRYlnTnWwY4Tpc44h[XO|YYm= M3TPe|k3KGh? NGSzTpVKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDEWU0yPDVicILvd5RifGViY3HuZ4VzKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJFk3KGi{LDDJR|UxRTBwMUGg{txO M3r3e|E3OTB5MUWy

... Click to View More Cell Line Experimental Data

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]


Kinase Assay:[1]
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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]
+ Expand
  • 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]
+ Expand
  • Animal Models: HCT-116 and PC-3 cells are injected s.c. into the right flank of nude mice.
  • Formulation: MLN8054 is dissolved in 10% hydroxypropyl-β-cyclodextrin with 5% sodium bicarbonate.
  • 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


CAS No. 869363-13-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID