AS-604850

ArtNr	S2681-25
Hersteller	Selleckchem
CAS-Nr.	648449-76-7
Menge	25 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 ml 2 mg 25 mg 5 mg 5 g
Kategorie	Neuroscience Neuroinflammation Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
Smiles	C1=CC2=C(C=C1C=C3C(=O)NC(=O)S3)OC(O2)(F)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	648449-76-7 '
Similar products	AS-604850
Lieferbar
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	285, 22
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
Concentrations	2.5 uM
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-1â€“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 2â€“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 2â€“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.
Solubility (25C)	DMSO 57 mg/mL, Water <1 mg/mL, Ethanol 5 mg/mL
Information	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.
Chemical Name	(Z)-5-((2, 2-difluorobenzo[d][1, 3]dioxol-5-yl)methylene)thiazolidine-2, 4-dione

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