产品说明书

MLN8054

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Chemical Structure| 869363-13-3 同义名 : -
CAS号 : 869363-13-3
货号 : A531108
分子式 : C25H15ClF2N4O2
纯度 : 99%+
分子量 : 476.862
MDL号 : MFCD11840561
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(41.94 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

15% Captisol+water 30 mg/mL suspension

生物活性
靶点

  • Aurora A

    Aurora A, IC50:4 nM

  • Aurora B

    Aurora B, IC50:172 nM
描述 MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase. It is over 40 times more selective for Aurora A than its family member Aurora B. In cultured human tumor cells, MLN8054 preferentially inhibits Aurora A over Aurora B. Treatment with MLN8054 leads to G2/M accumulation and spindle defects, and inhibits the proliferation of various cultured human tumor cell lines. MLN8054 effectively suppresses the growth of cells from different tissue origins, with IC50 values ranging from 0.11 to 1.43 μM[1]. Treatment of cultured human tumor cells with MLN8054 results in numerous morphological and biochemical changes associated with senescence[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
DU-145 prostate cancer cell Function assay 96 h Inhibitory concentration against DU-145 prostate cancer cell proliferation over 96 hr, IC50=0.11 μM 16107152
human Calu6 cells Proliferation assay 96 h Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.22 μM 17360485
human DLD1 cells Proliferation assay 96 h Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=1.43 μM 17360485
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00249301 Breast Neoplasm ... 展开 >> Colon Neoplasm Pancreatic Neoplasm Bladder Neoplasm 收起 << Phase 1 Terminated - United States, Tennessee ... 展开 >> The Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 收起 <<
NCT00652158 Advanced Malignancies Phase 1 Terminated - Spain ... 展开 >> Ciutat Sanitaria Vall d'Hebron Barcelona, Spain, 08035 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.49mL

2.10mL

1.05mL

20.97mL

4.19mL

2.10mL
参考文献

[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.