AS-604850 - Moligand™, 10mM in DMSO , Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit gamma, CAS No.648449-76-7, Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit gamma

CAS: 648449-76-7 Cat. No.: A408881 Molecular Weight: 285.22 EC Number: 636-351-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

AS-604850 is a selective, ATP-competitivePI3Kγinhibitor withIC50of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
In vitro

AS-604850 is ATP-competitive PI3Kγ inhibitor with K_i values of 0.18 μM. AS-604850 is 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) AS-604850 is capable of inhibiting C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 with 10 μM. AS-604850 blocks MCP-1-mediated chemotaxis in Pik3cg ^+/+ monocytes in a concentration- dependent manner, with an IC50 of 21 mM, but dosn\'t affect chemotaxis in Pik3cg^-/- cells, indicating that AS-604850 acts through PI3Kγ. AS-604850 diminishes glycochenodeoxycholate (GCDC) induced Akt-phosphorylation and apoptosis in rat hepatocytes. AS-604850 diminishes bile salt-induced apoptosis in HepG2 Ntcp and Huh7-Ntcp cells. AS604850 causes a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF).

In vivo

AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with a ED50 of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment.
Cell Data

cell lines：

Concentrations：2.5 μM

Incubation Time：2 - 4 hours

Powder Purity:≥99%

Specifications

Synonyms

(Z)-5-((2, 2-difluorobenzo[d][1, 3]dioxol-5-yl)methylene)thiazolidine-2, 4-dione

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit gamma

Names and Identifiers

• Isomeric SMILES: C1=CC2=C(C=C1/C=C/3\C(=O)NC(=O)S3)OC(O2)(F)F
• WGK Germany: 3
• Molecular Weight: 285.22
• Reaxy-Rn: 11711304
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11711304&ln=

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 Activities)

Discover Target: PIK3CG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 92 mg/mL (199.28 mM); Ethanol: 92 mg/mL (199.28 mM); DMSO: Insoluble