Home PI3K/Akt/mTOR PI3K inhibitor AS-252424

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AS-252424 PI3K inhibitor

Cat.No.S2671

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 PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 305.28

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Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=0.23 μM
THP1 cells Function assay Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=0.4 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 305.28 Formula

C14H8FNO4S

 Storage (From the date of receipt)
CAS No. 900515-16-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC(=C(C=C1F)O)C2=CC=C(O2)C=C3C(=O)NC(=O)S3

Solubility

In vitro
Batch:

DMSO : 61 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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
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Mechanism of Action

Targets/IC50/Ki
Casein Kinase 2 [1]
(Cell-free assay)
20 nM
PI3Kγ [1]
(Cell-free assay)
33 nM
PI3Kα [1]
(Cell-free assay)
935 nM
In vitro
AS-252424 is a furan-2-ylmethylene thiazolidenedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. This compound shows reduced potency on PI3Kα with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, this chemical doesn't show significant inhibit towards any of them at 10 μM except for CK2. It inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. This inhibitor 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] It 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 this compound significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3]
Kinase Assay
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 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]
References

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