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AS-604850 PI3K inhibitor

Cat.No.S2681

AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with an IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
AS-604850 PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 285.22

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Quality Control

Batch: S268101 DMSO]57 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Chemical Information, Storage & Stability

Molecular Weight 285.22 Formula

C11H5F2NO4S

 Storage (From the date of receipt)
CAS No. 648449-76-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC2=C(C=C1C=C3C(=O)NC(=O)S3)OC(O2)(F)F

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (199.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Mechanism of Action

Targets/IC50/Ki
PI3Kγ
0.25 μM
PI3Kα
4.5 μM
In vitro
AS-604850 is an ATP-competitive PI3Kγ inhibitor with Ki values of 0.18 μM. This compound is an isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα. (PI3Kα: IC50 = 4.5 μM, PI3Kγ and β: IC50 > 20μM) It is capable of inhibiting C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 of 10 μM. This chemical blocks MCP-1-mediated chemotaxis in Pik3cg+/+ monocytes in a concentration-dependent manner, with an IC50 of 21 mM, but doesn't affect chemotaxis in Pik3cg-/- cells, indicating that it acts through PI3Kγ. It diminishes glycochenodeoxycholate (GCDC) induced Akt-phosphorylation and apoptosis in rat hepatocytes. This compound diminishes bile salt-induced apoptosis in HepG2 Ntcp and Huh7-Ntcp cells. It causes a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF).
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 this compound or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded.
In vivo
AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with an ED50 of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg of this compound results in a 31% reduction of neutrophil recruitment.
References

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