MLN8054

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 20 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 MY\GeY5kfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKG2xdYPlJJJm[2:vYnnuZY51KEG3cn;yZUBCKGurbnHz[UBmgHC{ZYPz[YQhcW5iaX7z[YN1KFOoOTDj[YxteyCkeTDyZYRqd2GldHn2[UBndGG|aIDsZZRmKGG|c3H5MEBKSzVyPUSgcm0> NFzLVW4yPzN4MES4OS=>
human HCT116 cells NEXkUmVHfW6ldHnvckBie3OjeR?= NVziW21iUW6qaXLpeIlwdiCxZjDheZJwemFia3nuZZNmKEFiYYX0c5Bpd3OyaH;yfYxifGmxbjDheEBVOjh6IHnuJIh2dWGwIFjDWFEyPiClZXzsd{BjgSCrbX31co9ndHWxcnXzZ4Vv[2ViYX7hcJl{cXNuIFnDOVA:OC5yM{Sg{txO MmTDNlYyODF3NkS=
human HeLa cells M3TRNGZ2dmO2aX;uJIF{e2G7 NXzZTGVYOSCq NEXZcFVKdmirYnn0bY9vKG:oIFH1do9z[SCDIGTodlI5QCCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiMTDodkwhUUN3ME2wMlA{PCEQvF2= M1rxXVE4OzZyNEi1
human H460 cells NVPNbmN[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHP4c3k6PiCq NWD5N3NJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDCdoRWKGOnbHygdJJwdGmoZYLheIlwdiCHTFnTRUwhUUN3ME2wMlEyKM7:TR?= MoHJNVc{PjB2OEW=
human HT-29 cells M4\q[nBzd2yrZnXyZZRqd25iYYPzZZk> NUjjfJB{PCCmYYnz NIDt[ldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IESg[IF6eyCkeTDj[YxtfGm2ZYKgZZN{[XluIFnDOVA:OC5zNTFOwG0> Mm\4NVk1ODJ4M{O=
human Calu6 cells NF\1dldRem:uaX\ldoF1cW:wIHHzd4F6 NVnaXJNxQTZiaB?= NU\SbFJESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDZYx2PiClZXzsd{Bi\nSncjC5OkBpenNiYomgRpJlXSClZXzsJJBzd2yrZnXyZZRqd25iRVzJV2EtKEmFNUC9NE4zOiEQvF2= MlW0NVc{PjB2OEW=
human SKOV3 cells MoDYVJJwdGmoZYLheIlwdiCjc4PhfS=> NVrZVpdIQTZiaB?= M1P4NmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFLy[HUh[2WubDDwdo9tcW[ncnH0bY9vKEWOSWPBMEBKSzVyPUCuOVMh|ryP MkXUNVc{PjB2OEW=
human MCF7 cells NWTWc4lrWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkPLPVYhcA>? MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEK{ZGWgZ4VtdCCycn;sbYZmemG2aX;uJGVNUVODLDDJR|UxRTBwNkeg{txO M4rjNFE4OzZyNEi1
human MDAMB231 cells Mmj1VJJwdGmoZYLheIlwdiCjc4PhfS=> M1;C[Vk3KGh? NUfpWpdSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGFOSjJ|MTDj[YxteyCjZoTldkA6PiCqcoOgZpkhSnKmVTDj[YxtKHC{b3zp[oVz[XSrb36gSWxKW0FuIFnDOVA:OC55NDFOwG0> MoLrNVc{PjB2OEW=
human PC3 cells NGjFPXhRem:uaX\ldoF1cW:wIHHzd4F6 M{D4RVk3KGh? MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA6PiCqcoOgZpkhSnKmVTDj[YxtKHC{b3zp[oVz[XSrb36gSWxKW0FuIFnDOVA:OC55OTFOwG0> MYKxO|M3ODR6NR?=
human SW480 cells MnqyVJJwdGmoZYLheIlwdiCjc4PhfS=> M1H1[lk3KGh? MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNEiwJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCEcnTVJINmdGxicILvcIln\XKjdHnvckBGVEmVQTygTWM2OD1yLki2JO69VQ>? NYXoRmozOTd|NkC0PFU>
human DLD1 cells MoLBVJJwdGmoZYLheIlwdiCjc4PhfS=> MXm5OkBp MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESOREGgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEK{ZGWgZ4VtdCCycn;sbYZmemG2aX;uJGVNUVODLDDJR|UxRTFwNEOg{txO NXrWWGFkOTd|NkC0PFU>
DU-145 prostate cancer cell M{noNGZ2dmO2aX;uJIF{e2G7 MofmPVYhcA>? NGr2ZWpKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDEWU0yPDVicILvd5RifGViY3HuZ4VzKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJFk3KGi{LDDJR|UxRTBwMUGg{txO Mm\CNVYyODdzNUK=

... 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]

Protocol

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]
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  • 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]
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  • 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
Formula

C25H15ClF2N4O2

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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID