|9-环戊基-2-((2-甲氧基-4-((1-甲基哌啶-4-基)氧基)苯基)氨基)-7-甲基-7H-嘌呤-8(9H)-酮|CsnPharm

CAS No.: 1124329-14-1

9-Cyclopentyl-2-((2-methoxy-4-((1-methylpiperidin-4-yl)oxy)phenyl)amino)-7-methyl-7H-purin-8(9H)-one Catalog No. CSN15830

Synonyms: Mps1 Inhibitor III

AZ3146 is a selective and potent Mps1 inhibitor with IC50 value of 35 nM.

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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

靶点 Mps1

IC50:35nM
描述Monopolar spindle 1 (Mps1) is a spindle assembly checkpoint kinase that plays an essential role in the regulation of mitosis. AZ3146 inhibits human Mps1 with an IC50 value of 35 nM. In nocodazole-arrested Hela cells, AZ3146 at 1 – 30 μM inhibited the autophosphorylation of full-length Mps1. AZ3146 at 2 µM reduced the time for Hela cells to complete mitosis from 90 min to 32 min. Nearly 90% of AZ3146-treated Hela cells underwent abnormal mitoses with around 50% entering anaphase without aligning all the chromosomes and almost 30% exiting mitosis without chromosome segregation. AZ3146 at 2 µM also decreased the levels of Mad1 and Mad2 to 60% and 15%, respectively. The kinetochore recruitment of O-Mad2 in Hela cells was also blocked by at 2 µM AZ3146^[3]. The exposure of GSK923295, an inhibitor targeting the mitotic kinesin Cenp-E, combined with 2 µM AZ3146 induced whole chromosome aneuploidies in cells without causing DNA damage and significant disruption to the spindle^[4]. In AZ3146-resistent HCT116 cells created by long-term exposure of AZ3146, 24-hour incubation of 1 and 2 µM AZ3146 abolished the G₁ and G₂ - M peaks in the parental cell line and made them rapidly exit from mitosis^[5].
作用机制AZ3146 might inhibit Mps1 by promoting its kinetochore localization^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HCT116 cells	-	Function assay	-	Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132, IC50=0.72 μM	24256217
human HCT116 cells	-	Growth inhibition assay	72 h	Growth inhibition in human HCT116 cells after 72 hrs by MTT assay, GI50=1.2 μM	24256217
sf9 insect cells	-	Function assay	-	Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay, IC50=7 nM	24256217

动物研究
剂量
Mice: 50 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 50 mg/kg^[3] (i.p.)
给药途径	i.p.

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
- 2.2097 mL
- 11.0485 mL
- 22.0970 mL
- 5 mM
- 0.4419 mL
- 2.2097 mL
- 4.4194 mL
- 10 mM
- 0.2210 mL
- 1.1049 mL
- 2.2097 mL

技术信息

CAS号

1124329-14-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H32N6O3

运输

蓝冰

分子量

452.55

别名

Mps1 Inhibitor III

溶解度

DMSO	28.0 mg/mL (61.9 mM)
Water	Insoluble
Ethanol	90.0 mg/mL (198.9 mM)

动物实验配方

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9-Cyclopentyl-2-((2-methoxy-4-((1-methylpiperidin-4-yl)oxy)phenyl)amino)-7-methyl-7H-purin-8(9H)-one Catalog No. CSN15830

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