Molecular Formula | C12H7N3O2S
|
Molar Mass | 257.27 |
Density | 1.553±0.06 g/cm3(Predicted) |
Solubility | DMSO: soluble1mg/mL, clear (warmed) |
Appearance | powder |
Color | , faint red to orange to dark brown |
pKa | 6.02±0.20(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD11100415 |
Use | AS605240 |
In vitro study | AS-605240 inhibits PI3Kγ with an IC50 of 8 nM. AS-605240 is an ATP-competitive inhibitor of PI3Kγ with a Ki value of 7.8 nM. AS-605240 also inhibited PI3Kα,β, and δ, with IC50 values of 60,270, and 300 nM, respectively. AS-605240 inhibits c5a-mediated phosphorylation of PKB with an IC50 of 90 nM. 1 μm AS-605240 inhibited MCP-1 or CSF-1 of PKB phosphorylation induced by bone marrow mononuclear cells (BMDMs). 100 nM AS-605240 acts on the SC-CA1 synapse in the mouse, eliminating NMDAR LTD, without affecting mGluR LTD, and LTP. |
In vivo study | AS-605240 reduced neutrophil chemotaxis in a RANTES-induced murine model of peritonitis with an ED50 of 9.1 mg/kg. AS-605240 acts at a dose of 50 mg/kg on αcii-induced arthritis and protects it from αcii-IA symptoms. AS-605240 at a dose of 50 mg/kg also inhibited joint inflammation and injury in a collagen-induced arthritis mouse model. AS-605240 at a dose of 10 mg/kg in ob/ob mouse model of obesity-induced diabetes reduced blood glucose levels, significantly improved insulin sensitivity and glucose tolerance, and did not affect body weight. AS-605240 treatment at a dose of 30 mg/kg showed a better effect with only a slight effect on body weight. Moreover, AS-605240 reduced the amount of ATS and circulating levels MCP-1. |