1173900-33-8

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;(R)-2-(1-(7-Methyl-2-morpholino-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethylamino)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
• CAS NO: 1173900-33-8
• Molecular Formula: C₂₂H₂₄N₄O₄
• Molecular Weight: 408.45036
• EINECS: -0
• Product Categories: PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K
• Mol File: 1173900-33-8.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 635.5±65.0 °C(Predicted)
• Appearance: /
• Density: 1.36
• Solubility: insoluble in H2O; ≥20.4 mg/mL in DMSO; ≥6.36 mg/mL in EtOH
• PKA: 3.90±0.50(Predicted)
• CAS DataBase Reference: 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 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)
• EPA Substance Registry System: 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)

Safety Data

• Hazardous Substances Data: 1173900-33-8(Hazardous Substances Data)

Usage

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]

references

nylander s, kull b, bj?rkman 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.

Upstream product

• 885223-64-3 2-chloro-3-acetyl-5-methylpyridine 
• 88-65-3 2-bromobenzoic-acid 
• 1173900-36-1 2-[[(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid methyl ester 

Downstream Products

• 1622905-82-1 C₂₃H₂₇N₅O₅S 
• 1622905-80-9 C₂₂H₂₅N₅O₄ 

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