2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid
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
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
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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2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid(1173900-33-8)Related Product Information
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- 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-