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AS-604850

AS-604850

Item no.	S2681-25
Manufacturer	Selleckchem
CASRN	648449-76-7
Amount	25 mg
Category	Neuroscience Neuroinflammation Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	648449-76-7 '
Similar products	AS-604850
Available
Administration	Oral administration 30 or 15 minutes before injection of RANTES or thioglycollate
Animal Models	RANTES (0.5 mg/kg in 200 ml saline) or thioglycollate (40 ml/kg) are intraperitoneally injected to C3H mice to induce peritonitis mouse models
Cell lines	HepG2 Ntcp and Huh7-Ntcp cells
Chemical Name	(Z)-5-((2, 2-difluorobenzo[d][1, 3]dioxol-5-yl)methylene)thiazolidine-2, 4-dione
Concentrations	2.5 uM
Description	AS-604850 is a selective, ATP-competitive PI3Kgamma inhibitor with IC50 of 250 nM.
Dosages	0, 1, 3, 10 or 30 mg/kg for RANTES, 10 mg/kg for thioglycollate
Formulation	AS-604850 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
IC50	250 nM, 250 nM, 250 nM, 250 nM, 250 nM, 250 nM
In vitro	AS-604850 is ATP-competitive PI3Kgamma inhibitor with Ki values of 0.18 uM. AS-604850 is isoform selective inhibitor of PI3Kgamma with over 30-fold selectivity for PI3Kgamma and beta, and 18-fold selectivity over PI3Kalpha. (PI3Kalpha: IC50 = 4.5 uM, PI3Kgamma and beta: IC50 > 20uM) AS-604850 is capable of inhibiting C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 with 10 uM. 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 PI3Kgamma. [1] 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. [2] AS604850 causes a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF). [3]
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. [1]
Incubation Time	2 - 4 hours
Kinase Assay	In vitro PI3Kgamma Kinase Assay, Human PI3Kgamma (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM beta-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi gamma[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.
Method	Hepatocyte cultures are treated with diluent (DMSO), 25 uM TLC, 250 uM TCDC, 50 uM GCDC, or 50 ng/ml Fas for 2–4 hours HepG2-Ntcp and Huh7-Ntcp cells are treated with DMSO, 20 uM TLC, 75 uM TCDC or GCDC, 200 uM etoposide or 200 ng/ml TNFa plus 28 ng/ml actinomycin D for 2–4 hours. The number of apoptotic cells is determined morphologically using fluorescent staining and expressed as % of cells. Apoptosis is confirmed in human cell lines by determination of caspase-3/-7 activity and in rat hepatocytes by detection of the 17 kDa proteolytic cleavage fragment of caspase-3 by immunoblotting, equal protein loading is monitored by immunoblotting for actin.
Molecular Weight (MW)	285, 22
Picture ChemicalStructure Description	AS-604850 Chemical Structure
Picture Description 1	Data independently produced by Dr. Zhang of Tianjin Medical University, , AS-604850purchased from Selleck, After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of AS-604850 for 3h, followed by 20-minute stimolation of 100ng/ml EGF.
Solubility (25C)	DMSO 57 mg/mL, Water <1 mg/mL, Ethanol 5 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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Amount: 25 mg

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Delivery expected until 9/20/2024