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AS-252424

AS-252424 is a novel, potent and selective inhibitor of PI3Kγ with IC50 of 33 nM.

Catalog No.S2671

1 Reviews

: Tel: +1-832-582-8158[email protected]

AS-252424 Chemical Structure
Molecular Weight: 305.28

Validation & Quality Control

Customer Reviews(1) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

AS-252424 is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well)

Product Information

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1009	BEZ235 (NVP-BEZ235)	<1 mg/mL	1 mg/mL	<1 mg/mL
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S2671	AS-252424	<1 mg/mL	61 mg/mL	<1 mg/mL
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Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Tech Support & FAQs

Biological Activity

Description	AS-252424 is a novel, potent and selective inhibitor of PI3Kγ with IC50 of 33 nM.
Targets	PI3Kγ	CK2 (casein kinase 2)	PI3Kα
IC50	33 nM	20 nM	935 nM ^[1]
In vitro	AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kα with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 μM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. ^[1] AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. ^[2] A recent research indicates 100 nM of AS-252424 significantly reduces [Ca²⁺]i, I_Ca and Ca²⁺ transients in HL-1 cardiomyocytes. ^[3]
In vivo	Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%), almost matching the result observed in PI3Kγ-deficient mice. ^[1]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

In vitro PI3Kγ Kinase Assay	Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl₂, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na₃VO₄, 0.1% Na Cholate and 15 M ATP/100 nCi γ[³³]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded.

In vitro PI3Kγ Kinase Assay

Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl₂, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na₃VO₄, 0.1% Na Cholate and 15 M ATP/100 nCi γ[³³]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded.

Cell Assay: ^[1]

Cell lines	Raw-264 macrophage
Concentrations	0.01 nM to 0.1 μM
Incubation Time	5 minutes
Method	After 3 hours of starvation in serum-free medium, Raw-264 macrophages are pretreated with AS-252424 or DMSO for 30 minutes and stimulated for 5 minutes with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols.

Animal Study: ^[1]

Animal Models	Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
Formulation	AS-252424 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
Dosages	10 mg/kg
Administration	Oral administration 15 minutes before injection of thioglycollate

References

Chemical Information

Download AS-252424 SDF

Molecular Weight (MW)	305.28
Formula	C₁₄H₈FNO₄S
CAS No.	900515-16-4
Synonyms	N/A

Solubility (25°C) DMSO 61 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	(Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (1)

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Rating

Source

Dr. Zhang of Tianjin Medical University. AS-252424 purchased from Selleck

Method

Western blot

Cell Lines

A549 cells

Concentrations

0-10 μM

Incubation Time

3 h

Results

AS-252424 treatment resulted in a reduction of AKT phosphorylation.

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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