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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.
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Source | Int J Radiat Oncol Biol Phys (2011). Figure 1. MLN8054 |
| Method | Western blots | |
| Cell Lines | DU145 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 1 h | |
| Results | When MLN8054 was administered in combination with radiation, total Aurora-A remained elevated, but phospho-Aurora-A levels were reduced nearly to baseline levels, indicating abrogation of Aurora-A activity |
| 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 |
| Molecular Weight | 476.86 |
| Formula | C25H15ClF2N4O2 |
| CAS Number | 869363-13-3 |
| Solubility (25°C) | DMSO 24 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Aurora Kinase Products |
|---|
| Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. |
| Aurora Kinases-IN-4
Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). |
| Derrone
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. |
| CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
| Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
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