2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid

Definition

ChEBI: 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-9-pyrido[1,2-a]pyrimidinyl]ethyl]amino]benzoic acid is a pyridopyrimidine.

Biological Activity

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]

storage

Store at -20°C

References

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.