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AS-041164
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-041164图片
CAS NO:6318-41-8
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
AS-041164 是一种有效的、选择性的、具有口服活性的 PI3Kγ 异构体抑制剂，IC50 为 70 nM。
Cas No.6318-41-8
化学名5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione
Canonical SMILESO=C(/C(S1)=C/C2=CC=C3C(OCO3)=C2)NC1=O
分子式C11H7NO4S
分子量249.2
溶解度≤25mg/ml in DMSO;25mg/ml in dimethyl formamide
储存条件4°C, protect from light
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-041164 is a potent and selective PI3Kγ inhibitor with IC50 value of 0.07 μM [1].

The phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid and protein kinases regulating numerous biological processes, including cell growth, differentiation, survival, proliferation, migration and metabolism. PI3Kγ, a unique member of class IB, is activated exclusively by G-protein coupled receptor (GPCRs) and can specifically bind to adaptors unrelated to p85 proteins [2].

AS-041164 is a highly potent and selective PI3Kγinhibitor that inhibits PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with IC50 values of 240 nM, 1.45 μM, 70 nM and 1.70 μM, respectively [1].

In mice, orally administration of AS-041164 dose-dependently decreased r-hRANTES-induced neutrophil recruitment with ED50 value of 27.35 mg/kg. AS-041164 (30 mg/kg p.o.) also significantly reduced r-hRANTES-induced AKT phosphorylation. In a carrageenan-induced inflammation rat model, AS041164 at the dose of 100 mg/kg p.o significantly reduced paw thickness induced by carrageenan [1].

References:
[1].  Ferrandi C, Ardissone V, Ferro P, et al. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J Pharmacol Exp Ther. 2007 Sep;322(3):923-30.
[2].  Hirsch E, Ciraolo E, Ghigo A, et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacol Ther. 2008 May;118(2):192-205.