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Merck
CN

5.31976

MPS1 Inhibitor III, AZ3146

别名:

MPS1 Inhibitor III, AZ3146, AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146

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关于此项目

经验公式（希尔记法）:
C24H32N6O3
化学文摘社编号:
1124329-14-1
分子量:
452.55
MDL number:
MFCD18384959
UNSPSC Code:
12352200
NACRES:
NA.77

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InChI key

YUKWVHPTFRQHMF-UHFFFAOYSA-N

InChI

1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27)

SMILES string

N1(CCC(CC1)Oc2cc(c(cc2)Nc3nc4[n]([c]([n](c4cn3)C)=O)C5CCCC5)OC)C

assay

≥97% (HPLC)

form

powder

potency

~35 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

purple

solubility

DMSO: 5 mg/mL

Quality Level

100

相关类别

General description

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1; IC50 = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes
Reversible: yes

Packaging

Packaged under inert gas

Other Notes

Hewitt, L., et al. 2010. Jour. Cell Biol.190, 25.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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