现货大促销,价格低至8折起,量大更优惠,详细咨询客服
全部分类
全部分类
  • AS-604850
AS-604850的可视化放大

AS-604850

A selective inhibitor of PI3Kγ

原价
¥350-5687
价格
280-4550
AS-604850的二维码

所有产品仅用于科学研究,我们不为任何个人用途提供产品和服务

询价有惊喜,量大更优惠 点击这里给我发消息

  • 库存: 现货
可选包装 >>>
首页
  • 货号: ajci8402
  • CAS: 648449-76-7
  • 别名: 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮
  • 分子式: C11H5F2NO4S
  • 分子量: 285.22
  • 纯度: >98%
  • 溶解度: DMF: 20 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): .5 mg/ml,Ethanol: 5 mg/ml
  • 储存: Store at -20°C
  • 库存: 现货

Background

AS-604850 is a selective and ATP-competitive PI3Kγ inhibitor (IC50= 2.5 μM), with over 30-fold selectivity for PI3Kδ and PI3Kβ, and 18-fold selectivity over PI3Kα. [1]


PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt(PKB)/mTOR pathway.


In rat hepatocytes, AS-604850 pretreatment abolished GCDC-induced phosphorylation of Akt by 50% and inhibited apoptosis by reducing GCDC/TCDC/TLC-induced caspase-3 cleavage. [2] In PI3KCG-/-monocytes and THP-1 (human monocytic cell line), AS-604850 inhibited the PKB phosphorylation activated by MCP-1, it also blocked the MCP-1-mediated chemotaxis in a concentration dependent manner. In RAW264 mouse macrophages, C5a-mediated PKB phosphorylation was inhibited by AS-604850. [1]


In the thioglycollate-induced peritonitis model that induced multiple chemokine in vivo, oral administration of 10 mg/kg AS-604850 showed a 31% decrease of neutrophil recruitment. [1]

参考文献:
1.? Camps M, Rückle T, Ji H et al. Blockade of PI3K-gamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43.
2.? Hohenester S, Gates A, Wimmer R et al. Phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. J Hepatol. 2010 Nov;53(5):918-26.

动态评分

0.0

没有评分数据
没有评价数据
一键回到顶部
展开 收缩
安捷凯在线客服