Phosphatidylinositol 3-kinase （PI3K） catalyzes the phosphorylation of PI at the three position 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-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis. It inhibits human recombinant PI3Kγ， α， β， and δ in an ATP-competitive manner with IC50 values of 8， 60， 270， and 300 nM， respectively. AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo， AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg. AS-605240 （potassium salt） has improved solubility compared to AS-605240 （Item No. 10007707）.
产品描述
An orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis； inhibits human recombinant PI3Kγ， α， β， and δ in an ATP-competitive manner with IC50 values of 8， 60， 270， and 300 nM， respectively
