Research Area
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MLN8237 (Alisertib) Chemical Structure
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Biological Activity
MLN8237 (Alisertib) is a selective Aurora kinase A inhibitor with median IC50 of 61 nM. MLN8237 (Alisertib) is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the Aurora A kinase (serine/threonine protein kinase) with potential antineoplastic activity. MLN8237 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. After treatment in eight multiple myeloma cell lines with MLN8237 (Alisertib) (0.0001 μM – 4 μM) for 48 h, the affect of Aurora A kinase inhibition and a marked effect on both viability and proliferation (0.01 μM) was examined. Tumor burden was significantly reduced and overall survival was significantly increased in animals treated with 30 mg/kg MLN8237 (Alisertib). [1][2]
References on MLN8237 (Alisertib)
- [1] Pediatr Blood Cancer 2010;55:26–34
- [2] ACS CHEMICAL BIOLOGY 2010;5：536－576
Chemical Information
| Molecular Weight (WM): | 518.92 |
|---|---|
| Formula: | C27H20ClFN4O4 |
| CAS No.: | 1028486-01-2 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥44mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
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Selleck's high quality products have been used in several published research findings, including the following:
Drug-resistant Aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.
Uncovering new substrates for Aurora A kinase.
Emerging drugs for high-grade osteosarcoma.
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Inhibition of Aurora A (12.5 nM) by MLN8054 or MLN8237 was assessed in duplicate radiometric assays containing 100 ]M [γ-32P] ATP and quantified by p81 phosphocellulose assay and scintillation counting. Kinase activity is reported as a percentage of control calculated from duplicate incubations containing 2.5% (v/v) DMSO. IC50 values represent the mean ± SEM calculated from two independent experiments.
Inhibition of Aurora A (12.5 nM) by MLN8054 or MLN8237 was assessed in duplicate radiometric assays containing 100 ]M [γ-32P] ATP and quantified by p81 phosphocellulose assay and scintillation counting. Kinase activity is reported as a percentage of control calculated from duplicate incubations containing 2.5% (v/v) DMSO. IC50 values represent the mean ± SEM calculated from two independent experiments.
Data from [ACS Chem Biol 2010.April;5:563-576] MLN8237 (Alisertib) purchased from Selleck
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Click to enlarge
The effects of T217D and T217N Aurora A mutations were directly compared to WT Aurora A-expressing cells. Each well was treated with either DMSO or 500 nM MLN8054 (E), or 30 nM MLN8237 (F) on day one of the experiment and cells were cultured for 8 days, at which point they were fixed. For all colony assays, an area encompassing >90 % of the colonies per dish is shown. Similar results were seen in two independent duplicate experiments. - The effects of T217D and T217N Aurora A mutations were directly compared to WT Aurora A-expressing cells. Each well was treated with either DMSO or 500 nM MLN8054 (E), or 30 nM MLN8237 (F) on day one of the experiment and cells were cultured for 8 days, at which point they were fixed. For all colony assays, an area encompassing >90 % of the colonies per dish is shown. Similar results were seen in two independent duplicate experiments.
Data from [ACS Chem Biol 2010.April;5:563-576] MLN8237 (Alisertib) purchased from Selleck
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Click to enlarge
NUSAP mitotic phosphorylation at Ser 240 correlates with Aurora A activity. Protein samples of FLAG–NUSAP immunoprecipitated from I, M and MtMLN or with MtZM were analysed using LC-MS/MS, focusing on the predicted phosphorylated residue Ser 240. The histograms (A, B) show the calculated ratios based on peptides carrying the phosphorylated Ser 240 compared with all matched peptides containing this residue.
NUSAP mitotic phosphorylation at Ser 240 correlates with Aurora A activity. Protein samples of FLAG–NUSAP immunoprecipitated from I, M and MtMLN or with MtZM were analysed using LC-MS/MS, focusing on the predicted phosphorylated residue Ser 240. The histograms (A, B) show the calculated ratios based on peptides carrying the phosphorylated Ser 240 compared with all matched peptides containing this residue.
Data from [EMBO reports 2010.November;11:977-984] MLN8237 (Alisertib) purchased from Selleck
- Based on our preliminary data, I found MLN8237 and VX-680 have good effects in inhibiting Aurka-maintaining ESC self-renewal in mouse ES cells.
Dung-Fang LeeNYSCF-Stanley and Fiona Druckenmiller Fellow Black Family Stem Cell Research Institute Department of Gene and Cell Medicine Mount Sinai School of Medicine
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Inhibition of Aurora A (12.5 nM) by MLN8054 or MLN8237 was assessed in duplicate radiometric assays containing 100 ]M [γ-32P] ATP and quantified by p81 phosphocellulose assay and scintillation counting. Kinase activity is reported as a percentage of control calculated from duplicate incubations containing 2.5% (v/v) DMSO. IC50 values represent the mean ± SEM calculated from two independent experiments.
|
Data from [ACS Chem Biol 2010.April;5:563-576]
| The effects of T217D and T217N Aurora A mutations were directly compared to WT Aurora A-expressing cells. Each well was treated with either DMSO or 500 nM MLN8054 (E), or 30 nM MLN8237 (F) on day one of the experiment and cells were cultured for 8 days, at which point they were fixed. For all colony assays, an area encompassing >90 % of the colonies per dish is shown. Similar results were seen in two independent duplicate experiments. |
Data from [ACS Chem Biol 2010.April;5:563-576]
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