GLPBio

MLN8054

Catalog No.: GC12208Purity:>99.00%
COASDSData Sheet
An inhibitor of Aurora A kinase

Les produits sont exclusivement destinés à la recherche. Ils ne doivent pas être utilisés chez l’être humain. Nous ne vendons pas aux patients.

MLN8054
Cas No.: 869363-13-3
5mgIn Stock
$86.00
1
10mgIn Stock
$130.00
1
50mgIn Stock
$434.00
1
200mgIn Stock
$1,131.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

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  • Nature cover
    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    Science
    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    Cell Research
    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

Description

MLN8054 is a potent of Aurora A kinase (AAK) inhibitor consisting of a benzazepine core scaffold with a fused amino pyrimidine and an aryl carboxylic acid which represents an unprecedented kinase inhibitor framework. The inhibition of MLN8054 towards AAK is ATP-competitive, reversible and selective with an IC50 value of 4nM, which is more than 40-fold and 100-fold selective comparing to Aurora B kinase (IC50 = 175 nM) and a range of other kinases respectively. MLN8054 exerts antitumor activity against human tumor xenografts through AAK inhibition, which results in deactivation of Pt288, spindle defects, accumulation of G2/M, and apoptosis-induced cell death in tumor cells.

Reference

[1].Mark G. Manfredi, Jeffery A. Ecsedy, Kristan A. Meetze, Suresh K. Balani, Olga Burenkova. Wei Chen, Katherine M. Galvin, Kara M. Hoar, Jessica J. Huck, Patrick J. LeRoy, Emily T. Ray, Todd B. Sells, Bradley Stringer, Stephen G. Stroud, Tricia J. Vos, Gabriel S. Weatherhead, Deborah R. Wysong, Mengkun Zhang, Joseph B. Bolen, and Christopher F. Claiborne. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of aurora A kinase. PNAS 2007; 104(10): 4106-4111

Protocole (Protocol)

Cell experiment:

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].

Animal experiment:

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].

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.
[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.

Documents produit (Product Documents)

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Propriétés chimiques (Chemical Properties)

N° CAS
869363-13-3
Nom chimique
4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid
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
Formule moléculaire
C25H15ClF2N4O2
Masse moléculaire
476.86
Solubilité
≥ 39.05 mg/mL in DMSO
Conservation
Store at -20°C
Conseils généraux
Choisissez un solvant adapté selon les données de solubilité du produit. Après préparation, répartissez la solution mère en aliquotes afin d’éviter les cycles répétés de congélation-décongélation.
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Conditions d’expédition
Les échantillons d’évaluation sont expédiés avec des blocs réfrigérants. Les autres formats sont expédiés à température ambiante ou, sur demande, avec des blocs réfrigérants.

Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité

g/mol

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