| 分子量(MW): | 518.92 | |
|---|---|---|
| 化学式: | C27H20ClFN4O4 | |
| 溶解度: | DMSO ≥44mg/mL Water <1mg/mL Ethanol <1mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 1028486-01-2 |
MLN8237是Aurora A选择性的次代YZ剂，在酶活实验和细胞实验时IC50都为1nM。在异种移植鼠模型中MLN8237YZ肿瘤生长。[1]MLN8237YZCCRF-CEM细胞生长，实验72小时时IC50达到18.9nM。MLN8237YZMT-4细胞生长，实验72小时时IC50达到7.2 nM。MLN8237YZHUT-102细胞生长,实验72小时时IC50达到6.8 nM。[2] MLN8237可以口服且很快被吸收，可以降低苯二氮等镇静药对神经系统的影响。恶性血液肿瘤是严重影响血液，，淋巴结的一类癌症。MLN8237用于ZL恶性血液肿瘤已经处于一期阶段。[3]MLN8237Z初是由Millennium制药公司研究的。
[1] Güllü Görgün, et al. Blood, June 24, 2010 vol. 115 no. 25 5202-5213
[2] Mariko Tomita,et al. Cancer Science ,Volume 101, Issue 5, pages 1204–1211, May 2010
[3] http://clinicaltrials.gov/ct2/results?term=MLN8237
| 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.
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| 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. | |
| 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.
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