AS 604850 Chemical Properties

Density 

1.71

storage temp. 

2-8°C

solubility 

DMSO: >10mg/mL

form 

solid

pka

7.07±0.20(Predicted)

color 

off-white

Safety Information

Hazard Codes 

Xi

Risk Statements 

43

Safety Statements 

36/37

WGK Germany 

3

AS 604850 Usage And Synthesis

Description

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P₂ and PtdIns-(3,4,5)-P₃. PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC₅₀ values of 0.25, >20, >20, and 4.5 μM for the human recombinant γ, δ, β, and α isoforms, respectively. AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC₅₀ value of 21 μM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED₅₀ value of 42.4 mg/kg.

Uses

AS-604850 is a selective and ATP-competitive phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor.

References

1. camps m, rückle t, ji h et al. blockade of pi3k-gamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. nat med. 2005 sep;11(9):936-43.2. hohenester s, gates a, wimmer r et al. phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. j hepatol. 2010 nov;53(5):918-26.

AS 604850(648449-76-7)Related Product Information

• Thianaphthene
• DIBENZAZEPINE
• Dibenzothiophene
• PD 173074
• Selumetinib
• Nintedanib
• PHT-427
• OSU-03012 (AR-12)
• AT9283