AS-604850

648449-76-7

285.22

DMSO : 250 mg/mL (876.52 mM; Need ultrasonic)

PI3K/Akt/mTOR

AS-604850 is a potent, selective and ATP-competitive PI3Kgamma inhibitor with an IC₅₀ value of 0.25 uM and a K_i value of 0.18 uM. AS-604850 shows isoform selective inhibitor of PI3Kgamma with over 30-fold selectivity for PI3Kdelta and beta, and 18-fold selectivity over PI3Kalpha, respectively^[1]. In Vitro: AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC₅₀ of 10 uM in RAW264 mouse macrophages^[1].
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg^+/+ or Pik3cg^-/- mice^[1].
AS-604850 (0-30 uM; 15 minutes; primary monocytes from Pik3cg^+/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3alpha andbeta in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg^+/+ mice^[1]. 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].