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AS-041164

Catalog No.GC11910

L'AS-041164 est un inhibiteur d'isoforme PI3Kγ puissant, sélectif et actif par voie orale avec une IC50 de 70 nM.

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AS-041164 Chemical Structure

Cas No.: 6318-41-8

Taille Prix Stock Qté
5mg
52,00 $US
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10mg
81,00 $US
En stock
25mg
153,00 $US
En stock
50mg
255,00 $US
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 6318-41-8 SDF
Chemical Name 5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione
Canonical SMILES O=C(/C(S1)=C/C2=CC=C3C(OCO3)=C2)NC1=O
Formula C11H7NO4S M.Wt 249.2
Solubility ≤25mg/ml in DMSO;25mg/ml in dimethyl formamide Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.0128 mL 20.0642 mL 40.1284 mL
5 mM 0.8026 mL 4.0128 mL 8.0257 mL
10 mM 0.4013 mL 2.0064 mL 4.0128 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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