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AZD6482

Catalog No.
A5478
PI3Kβ inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$149.00
In stock
5mg
$120.00
In stock
25mg
$360.00
In stock
100mg
$980.00
In stock

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Email: [email protected]

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Background

AZD6428 is a potent, selective and ATP-competitive PI3Kβ inhibitor. IC50 are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, respectively.

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.

In vitro, AZD6482 inhibited insulin-activated uptake of human adpocyte glucose (IC50=4.4 μm). A full anti-thrombotic response with no increased bleeding or blood loss was observed in dog treated with AZD6482 in vivo. It also showed good tolerance in a three-hour AZD6482 infusion in healthy volunteers. There was an approx.10-20% rise at 5.3 μm (highest plasma concentration) according to the homeostasis model analysis index. [1]

Reference:
Nylander S, Kull B, Björkman JA et al.  Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt408.45
Cas No.1173900-33-8
FormulaC22H24N4O4
Solubility≥20.4mg/mL in DMSO, ≥6.36 mg/mL in EtOH,insoluble in H2O
Chemical Name2-[[(1R)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoic acid
SDFDownload SDF
Canonical SMILESCC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Protocol

Cell experiment [1]:

Cell lines

Primary human insulin sensitive adipocytes

Preparation method

The solubility of this compound in DMSO is >20.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.4-1 μM

Applications

AZD6482 is a novel isoform-selective inhibitor of PI3Kβ (phosphoinositide 3-kinase) that blocks the interaction of the enzyme with ATP. AZD6482 concentration-dependently inhibited insulin-induced glucose uptake by human adipocytes. Taken together, AZD6482 inhibited platelet aggregation induced by low agonist concentrations.

Animal experiment [2]:

Animal models

Folts dog model

Dosage form

intravenously (i.v.) over 30-min periods (bolus 0.03–1.3 μg kg-1) and (infusion 0.005–0.24 μg kg min-1)

Application

In vivo in dog, AZD6482 induced a concentration-dependent anti-thrombotic effect in vivo in the dog [abolition of the CFRs(cyclic flow reductions)]. AZD6482 left the shear induced primary platelet aggregation intact but inhibits secondary platelet aggregation, produced a complete antithrombotic effect without significantly compromising hemostasis as no increase in bleeding time or blood loss was seen at plasma exposure that achieved a full anti-thrombotic effect.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Nylander S, Kull B, Bjrkman JA ., et al.Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.

Biological Activity

Description AZD6482 is an inhibitor of PI3Kβ with an IC50 value of 10 nM.
Targets PI3Kβ PI3Kδ DNA-PK PI3Kα PI3Kγ  
IC50 10 nM 80 nM 420 nM 870 nM 1090 nM  

Quality Control

Quality Control & MSDS

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Chemical structure

AZD6482