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

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

Product Name:
2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid
Synonyms:
  • 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid
  • AZD 6482
  • AZD6482(PI3-kinase β inhibitor)
  • AZD-6482/AZD6482
  • AZD6482(r)
  • (R)AZD64822-[[(1R)-1-[7-Methyl-2-(4-Morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyriMidin-9-yl]ethyl]aMino]benzoic acid
  • KIN-193
  • 2-[[(1R)-1-[7-Methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid AZD 6482
CAS:
1173900-33-8
MF:
C22H24N4O4
MW:
408.45
Product Categories:
  • Akt
  • mTOR
  • PI3K/Akt/mTOR
  • Inhibitors
  • PI3K
Mol File:
1173900-33-8.mol
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2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid Chemical Properties

Boiling point:
635.5±65.0 °C(Predicted)
Density 
1.36
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥20.4 mg/mL in DMSO; ≥6.36 mg/mL in EtOH
form 
solid
pka
3.90±0.50(Predicted)
color 
White to light yellow
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2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid Usage And Synthesis

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.

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

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