Home >> AZ3146
Related Products
AZ3146 Mps1 inhibitor,potent and selective

Catalog No.A8372
Size Price Stock Qty
10mM (in 1mL Ethanol)
$94.00
In stock
10mg
$85.00
In stock
50mg
$250.00
In stock
100mg
$450.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

AZ3146

Biological Activity

Description AZ3146 is a selective inhibitor of Mps1 with IC50 of ~35 nM.
Targets Mps1          
IC50 ~35 nM          

AZ3146 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

AZ3146 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1124329-14-1 SDF Download SDF
Synonyms AZ 3146; AZ-3146
Chemical Name 9-cyclopentyl-2-[2-methoxy-4-(1-methylpiperidin-4-yl)oxyanilino]-7-methylpurin-8-one
Canonical SMILES CN1CCC(CC1)OC2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCCC5)OC
Formula C24H32N6O3 M.Wt 452.55
Solubility ≥15.3mg/mL in Ethanol Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

AZ3146 is a potent and selective Monopolar Spindle 1 (Mps1) kinase inhibitor with IC50 value of 35 nM. AZ3146 acts by interfering with chromosome alignment and overriding the spindle assembly checkpoint.

MPS1 protein kinases play important roles in different steps in mitosis including chromosome attachment and functions at the centrosomes. Additionally, they are also involved in regulation of development and in multiple signaling pathways after mitosis.

In cellular culture, if Mps1 is inhibited by AZ3146 before mitotic entry, this inhibition abloshed the subsequent recruitment of Mad1 and Mad2 to kinetochores. However, if cells were treated with AZ3146 after mitotic entry, the Mad1-C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. , AZ3146 interferes with chromosome alignment and overrides spindle assembly checkpoint1.

Regarding the effect of AZ3146 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.

Reference:
1.   Hewitt L, Tighe A, Santaguida S, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. The Journal of cell biology.2010;190(1):25-34.