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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6318-41-8
Sample solution is provided at 25 µL, 10mM.
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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.
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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