AS-252424

Catalog No.S2671

For research use only.

AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.

AS-252424 Chemical Structure

CAS No. 900515-16-4

Selleck's AS-252424 has been cited by 20 publications

Purity & Quality Control

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Biological Activity

Description AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
Targets
Casein Kinase 2 [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
20 nM 33 nM 935 nM
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, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Raw264 macrophage MofhSpVv[3Srb36gZZN{[Xl? M1XiS2lvcGmkaYTpc44hd2ZiQ{XhMY1m\GmjdHXkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIGLhe|I3PCCvYXPyc5Bp[WenLDDJR|UxRTBwMkOg{txO NX;I[ItWOTZ5OEm3OFI>
THP1 cells NWDaXItoTnWwY4Tpc44h[XO|YYm= NX6xW45sUW6qaXLpeIlwdiCxZjDNR3AyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0xNjRizszN MlPXNVY4QDl5NEK=
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]

Protocol (from 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.

Cell Research:[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 Research:[1]
  • Animal Models: Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
  • Dosages: 10 mg/kg
  • Administration: Oral administration 15 minutes before injection of thioglycollate

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 305.28
Formula

C14H8FNO4S

CAS No. 900515-16-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1F)O)C2=CC=C(O2)C=C3C(=O)NC(=O)S3

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

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Tech Support

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

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