中文名 | 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 |
英文名 | AS-604850 |
别名 | 5-(2,2-二氟-苯唑[1,3]二氧-5-基亚甲基)-噻唑烷-2,4-二酮 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 |
英文别名 | AS 604850 AS-604850 PI 3-Kγ Inhibitor II PI 3-Kinase Inhibitor (AS604850) B-0302 5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione (Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione PI3Kγ inhibitor, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione |
CAS | 648449-76-7 |
化学式 | C11H5F2NO4S |
分子量 | 285.22 |
密度 | 1.71 |
溶解度 | DMSO: >10 mg/mL |
酸度系数 | 7.07±0.20(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | off-white |
MDL号 | MFCD19705528 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 43 - 与皮肤接触可能致敏。 |
安全术语 | 36/37 - 穿戴适当的防护服和手套。 |
WGK Germany | 3 |
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