生物活性 | |||
---|---|---|---|
靶点 |
|
||
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 |
---|