5-[(2,2-二氟-1,3-苯并二恶茂-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,648449-76-7,结构式](https://www.chemicalbook.com/CAS/GIF/648449-76-7.gif)
- CAS号:648449-76-7
- 英文名:AS 604850
- 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
- CBNumber:CB5972768
- 分子式:C11H5F2NO4S
- 分子量:285.22
- MOL File:648449-76-7.mol
- 密度 :1.71
- 储存条件 :2-8°C
- 溶解度 :DMSO: >10mg/mL
- 形态 :solid
- 酸度系数(pKa) :7.07±0.20(Predicted)
- 颜色 :off-white
5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮性质、用途与生产工艺
- 生物活性 AS-604850 是一种有效的，具有选择性的和 ATP 竞争性的 PI3Kγ 抑制剂，IC50 值为 0.25 μM，Ki 值为 0.18 μM。AS-604850 是 PI3Kγ 的同工型选择性抑制剂，对 PI3Kγ 的选择性是 PI3Kδ/β 的 30 倍以上，是 PI3Kα 的 18 倍以上。
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靶点
PI3Kγ
0.25 μM (IC 50 )
PI3Kγ
0.18 μM (Ki)
PI3Kα
4.5 μM (IC 50 )
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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.
- 更新日期：2024/08/19
- 产品编号：HY-13531
- 产品名称：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
- CAS编号：648449-76-7
- 包装：5mg
- 价格：579元
- 更新日期：2024/08/19
- 产品编号：HY-13531
- 产品名称：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
- CAS编号：648449-76-7
- 包装：10 mM * 1 mLin DMSO
- 价格：715元
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6913
- 优势度：91
