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MLN8054

Cat. No. M1751

MLN8054 Structure
Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 600 In stock
100mg USD 850 In stock
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Quality Control
Biological Activity

MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of Aurora with IC50s of 0.004uM and 0.172uM. for Aurora A and Aurora B.Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation.

Protocol
Cell Experiment
Cell lines HCT116, PC-3, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460 and SKOV-3 cell lines
Preparation method Cell Viability Analysis. Human tumor cell lines obtained from the American Type Culture Collection were grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, was added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution was 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 were treated with MLN8054 for 96 h at 37°C in a humidified cell culture chamber. Cell viability in each cell line was measured by using the Cell Proliferation ELISA, BrdU colorimetric kit according to the manufacturer's recommendations (Roche).
Concentrations 0.04~10 mM
Incubation time 96 hr
Animal Experiment
Animal models Female (HCT-116) and male (PC3) athymic nude NCR (nu/nu) mice
Formulation 10% hydroxypropyl-β-cyclodextrin (Sigma) with 5% sodium bicarbonate
Dosages 10 or 30 mg/kg BID or 30mg/kg QD for 21 consecutive days
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 476.86
Formula C25H15ClF2N4O2
CAS Number 869363-13-3
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Molecular dynamics and free energy studies on Aurora kinase A and its mutant bound with MLN8054: insight into molecular mechanism of subtype selectivity.
Yang Y et al. Mol Biosyst. 2012 Sep 18. PMID: 22990663.

Combined inhibition of cellular pathways as a future therapeutic option in fatal anaplastic thyroid cancer.
Wunderlich A et al. Endocrine. 2012 Apr 5. PMID: 22477151.

MLN8054, a small molecule inhibitor of aurora kinase a, sensitizes androgen-resistant prostate cancer to radiation.
Moretti L et al. Int J Radiat Oncol Biol Phys. 2011 Jul 15;80(4):1189-97. PMID: 21514073.

Phase I assessment of new mechanism-based pharmacodynamic biomarkers for MLN8054, a small-molecule inhibitor of Aurora A kinase.
Chakravarty A et al. Cancer Res. 2011 Feb 1;71(3):675-85. PMID: 21148750.

Phase I study of the selective Aurora A kinase inhibitor MLN8054 in patients with advanced solid tumors: safety, pharmacokinetics, and pharmacodynamics.
Macarulla T et al. Mol Cancer Ther. 2010 Oct;9(10):2844-52. PMID: 20724522.

Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.
Sloane DA et al. ACS Chem Biol. 2010 Jun 18;5(6):563-76. PMID: 20426425.

MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo.
Huck JJ et al. Mol Cancer Res. 2010 Mar;8(3):373-84. PMID: 20197380.

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Manfredi MG, et al. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. PMID: 17360485.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MLN8054 supplier, Aurora Kinase, inhibitors

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