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 44 publications

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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 NILWc4ZHfW6ldHnvckBie3OjeR?= MlPUTY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCDdYLvdoEhSSCtaX7hd4Uh\XiycnXzd4VlKGmwIHnud4VkfCCVZkmgZ4VtdHNiYomgdoFlcW:jY4TpeoUh\myjc3jwcIF1\SCjc4PhfUwhUUN3ME20JI5O NWP3UYpSOTd|NkC0PFU>
human HCT116 cells MU\GeY5kfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGG3cn;yZUBscW6jc3WgRUBifXSxcHjvd5Bpd3K7bHH0bY9vKGG2IGSyPFghcW5iaIXtZY4hUEOWMUG2JINmdGy|IHL5JIludXWwb3\seY9z\XOlZX7j[UBidmGueYPpd{whUUN3ME2wMlA{PCEQvF2= MnG5NlYyODF3NkS=
human HeLa cells MojiSpVv[3Srb36gZZN{[Xl? NG\0TVgyKGh? MYXJcohq[mm2aX;uJI9nKEG3cn;yZUBCKFSqckK4PEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhOSCqcjygTWM2OD1yLkCzOEDPxE1? NY\2O|V5OTd|NkC0PFU>
human H460 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 Ml;HPVYhcA>? MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEh2NkCgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEK{ZGWgZ4VtdCCycn;sbYZmemG2aX;uJGVNUVODLDDJR|UxRTBwMUGg{txO MYixO|M3ODR6NR?=
human HT-29 cells M37ZVXBzd2yrZnXyZZRqd25iYYPzZZk> M1jkb|Qh\GG7cx?= M1n3ZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IHPlcIx1cXSncjDhd5NigSxiSVO1NF0xNjF3IN88US=> M3T0fFE6PDB{NkOz
human Calu6 cells NWTkRoFkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGrON2M6PiCq MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOjbIW2JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCEcnTVJINmdGxicILvcIln\XKjdHnvckBGVEmVQTygTWM2OD1yLkKyJO69VQ>? NYPsWJU6OTd|NkC0PFU>
human SKOV3 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 M2fJdFk3KGh? NVrXeGQ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{Bi\nSncjC5OkBpenNiYomgRpJlXSClZXzsJJBzd2yrZnXyZZRqd25iRVzJV2EtKEmFNUC9NE42OyEQvF2= MV:xO|M3ODR6NR?=
human MCF7 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 MkPCPVYhcA>? Mlm3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCEcnTVJINmdGxicILvcIln\XKjdHnvckBGVEmVQTygTWM2OD1yLk[3JO69VQ>? NInoUHMyPzN4MES4OS=>
human MDAMB231 cells NIraNlVRem:uaX\ldoF1cW:wIHHzd4F6 M2q3bFk3KGh? NWfzNXhUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGFOSjJ|MTDj[YxteyCjZoTldkA6PiCqcoOgZpkhSnKmVTDj[YxtKHC{b3zp[oVz[XSrb36gSWxKW0FuIFnDOVA:OC55NDFOwG0> NGKzXpAyPzN4MES4OS=>
human PC3 cells MnXtVJJwdGmoZYLheIlwdiCjc4PhfS=> Ml\JPVYhcA>? NVuyZmg2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFLy[HUh[2WubDDwdo9tcW[ncnH0bY9vKEWOSWPBMEBKSzVyPUCuO|kh|ryP MYixO|M3ODR6NR?=
human SW480 cells M3X1cXBzd2yrZnXyZZRqd25iYYPzZZk> NIHOcoE6PiCq MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNEiwJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCEcnTVJINmdGxicILvcIln\XKjdHnvckBGVEmVQTygTWM2OD1yLki2JO69VQ>? MVexO|M3ODR6NR?=
human DLD1 cells MnvzVJJwdGmoZYLheIlwdiCjc4PhfS=> NIfMWFU6PiCq NIDTSmlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTMSFEh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFLy[HUh[2WubDDwdo9tcW[ncnH0bY9vKEWOSWPBMEBKSzVyPUGuOFMh|ryP MU[xO|M3ODR6NR?=
DU-145 prostate cancer cell Mmj4SpVv[3Srb36gZZN{[Xl? M2XKR|k3KGh? NF7KS|FKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDEWU0yPDVicILvd5RifGViY3HuZ4VzKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJFk3KGi{LDDJR|UxRTBwMUGg{txO M3XjWlE3OTB5MUWy
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
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.

Solubility (25°C)

In vitro

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

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)

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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.

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Molarity Calculator

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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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