648449-76-7
648449-76-7 结构式
基本信息
5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮
AS 604850
AS-604850
AS 604850
AS 604850 USP/EP/BP
PI 3-Kγ Inhibitor II
AS604850
AS 604850
AS-604850
PI 3-Kinase Inhibitor (AS604850)
PI 3-Kinase Inhibitor (AS604850) B-0302
PI 3-Kγ Inhibitor II - CAS 648449-76-7 - Calbiochem
5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione
常见问题列表
|
PI3Kγ 0.25 μM (IC 50 ) |
PI3Kγ 0.18 μM (Ki) |
PI3Kα 4.5 μM (IC 50 ) |
AS-604850 inhibits C5a-mediated PKB phosphorylation with an
IC
50
of 10 μM in RAW264 mouse macrophages.
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.
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg
+/+
mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ 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.
Western Blot Analysis
| Cell Line: | Primary monocytes from Pik3cg +/+ mice |
| Concentration: | 0 μM, 1 μM, 3 μM, 10 μM, 30 μM |
| Incubation Time: | 15 minutes |
| Result: | Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice. |
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 ED 50 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.
| Animal Model: | Balb/C or C3H mice with human recombinant RANTES or thioglycollate |
| 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 ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |