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AS-604850
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AS-604850图片
CAS NO:648449-76-7
包装与价格：
包装价格(元)
2mg电议
5mg电议
25mg电议
100mg电议

产品介绍
AS-604850 是一种有效的、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 显示 PI3Kγ 的异构体选择性抑制剂，对 PI3Kδ 和 β 的选择性分别超过 30 倍，对 PI3Kα 的选择性高出 18 倍。
Cas No.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
化学名5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
Canonical SMILESC1=CC2=C(C=C1C=C3C(=O)NC(=O)S3)OC(O2)(F)F
分子式C11H5F2NO4S
分子量285.22
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
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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]

References:
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.