Cat. No. Name Size Price Add Cart
KI3490AS-604850QuoteQuote

Chemical Characteristic

Product NameAS-604850
CAS No.648449-76-7
Molecular Weight 285.225
FormulaC11H5F2NO4S
Chemical Name(Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione
SmilesS1C(=O)NC(=O)/C/1=C\c1cc2OC(Oc2cc1)(F)F
Chemical Structure

Biological activities

AS-604850 is a selective inhibitor of PI3Kγ. In vitro, AS-604850 is ATP-competitive PI3Kγ inhibitor with a Ki value of 0.18 µM. AS-604850 inhibits C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 of 10 µM. Acting through PI3Kγ, AS-604850 blocks MCP-1-mediated chemotaxis in Pik3cg+/+ monocytes in a concentration-dependent manner.[1] AS-604850 diminishes bile salt-induced apoptosis in HepG2-Ntcp and Huh7-Ntcp cells and induces a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF). In rat hepatocytes, AS-604850 diminishes glycochenodeoxycholate (GCDC) induced Akt-phosphorylation and apoptosis. In vivo, AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with a ED50 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.[2] AS-604850 shows anti-inflammatory activity in animal models of chronic inflammation.[3]

Protocols

In vitro, AS-604850 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.[1]

References

[1] Pinson J A, et al. Thiazolidinedione??ased PI3Kα Inhibitors: An Analysis of Biochemical and Virtual Screening Methods. ChemMedChem. 2011, 6(3): 514-522.
[2] Hasan A M, et al. Phosphoinositide 3-kinase γ mediates chemotactic responses of human eosinophils to platelet-activating factor. International immunopharmacology. 2010, 10(9): 1017-1021.
[3] Camps M,et al. Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nature medicine. 2005, 11(9): 936-943.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.