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CAS No.: 869363-13-3

MLN8054 Catalog No. CSN12363

Synonyms: Mln8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM and exhibits more than 40-fold selective for Aurora A than Aurora B.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM and exhibits more than 40-fold selective for Aurora A than Aurora B.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
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 ... more >> Colon Neoplasm Pancreatic Neoplasm Bladder Neoplasm Collapse <<	Phase 1	Terminated	-	United States, Tennessee ... more >> The Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 Collapse <<
NCT00652158	Advanced Malignancies	Phase 1	Terminated	-	Spain ... more >> Ciutat Sanitaria Vall d'Hebron Barcelona, Spain, 08035 Collapse <<

参考文献

[1] Moretti L, Niermann K, et al. MLN8054, a small molecule inhibitor of aurora kinase a, sensitizes androgen-resistant prostate cancer to radiation. Int J Radiat Oncol Biol Phys. 2011 Jul 15;80(4):1189-97.
[2] Manfredi MG, Ecsedy JA, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0970 mL
- 10.4852 mL
- 20.9704 mL
- 5 mM
- 0.4194 mL
- 2.0970 mL
- 4.1941 mL
- 10 mM
- 0.2097 mL
- 1.0485 mL
- 2.0970 mL

技术信息

CAS号

869363-13-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H15ClF2N4O2

运输

蓝冰

分子量

476.86

别名

Mln8054

溶解度

DMSO	95.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

15% Captisol+water

30 mg/mL

suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
human HCT116 cells	-	Function assay	-	Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis, IC50=0.034 μM	26101564
human HeLa cells	-	Function assay	1 h	Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr, IC50=0.034 μM	17360485
human HT-29 cells	-	Proliferation assay	4 days	Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay, IC50=0.15 μM	19402633
human MCF7 cells	-	Proliferation assay	96 h	Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.67 μM	17360485
human MDAMB231 cells	-	Proliferation assay	96 h	Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.74 μM	17360485
human PC3 cells	-	Proliferation assay	96 h	Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.79 μM	17360485
human SKOV3 cells	-	Proliferation assay	96 h	Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.53 μM	17360485
human SW480 cells	-	Proliferation assay	96 h	Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.86 μM	17360485
Sf9 cells	-	Function assay	-	Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay, IC50=4 nM	17360485

MLN8054 Catalog No. CSN12363

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