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].
MLN8054 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
human H460 cells
Proliferation assay
96 h
Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.11 μM
17360485
MLN8054 动物研究
Animal study
In HCT-116 tumor-bearing mice, treatment with MLN8054 inhibits tumor growth in a dose-dependent manner. MLN8054 is generally well-tolerated. It also inhibits the growth of PC-3 tumor xenografts in nude mice. Treatment with MLN8054 suppresses Aurora A in vivo, mitotic cell accumulation, and apoptosis[1]. At a dosage of 30 mg/kg, MLN8054 selectively inhibits the activity of Aurora A kinase. In HCT116 tumor tissues, at this dosage, MLN8054 has been demonstrated to inhibit the autophosphorylation of Aurora A and induce an increase in the Aurora B substrate pHisH3[2].
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