Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  PI3K / Akt / mTOR >  PI3K inhibitor >  AS 604850

AS 604850

Basic information Safety Supplier Related

AS 604850 Basic information

Product Name:
AS 604850
Synonyms:
  • AS 604850
  • PI3Kγ inhibitor, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
  • PI 3-Kinase Inhibitor (AS604850) B-0302
  • (Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione
  • 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
  • AS-604850;AS 604850
  • PI 3-Kγ Inhibitor II
  • 5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione
CAS:
648449-76-7
MF:
C11H5F2NO4S
MW:
285.22
Product Categories:
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
Mol File:
648449-76-7.mol
More
Less

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
More
Less

Safety Information

Hazard Codes 
Xi
Risk Statements 
43
Safety Statements 
36/37
WGK Germany 
3
More
Less

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.

in vivo

AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment[1].

Animal Model:Balb/C or C3H mice with human recombinant RANTES or thioglycollate[1]
Dosage:10 mg/kg, 30 mg/kg or 100 mg/kg
Administration:Oral administration; for 4.5 or 4.25 hours
Result:Reduced RANTES-induced peritoneal neutrophil recruitment with an ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment.

IC 50

PI3Kγ: 0.25 μM (IC50); PI3Kγ: 0.18 μM (Ki); PI3Kα: 4.5 μM (IC50)

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 604850Supplier

J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Email
sales@trio-pharmatech.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Email
anhua.mao@aladdin-e.com
More
Less

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