AS-252424

ArtNr	S2671-25
Hersteller	Selleckchem
CAS-Nr.	900515-16-4
Menge	25 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 ml 2 mg 25 mg 5 mg 5 g
Kategorie	Oncology Food Safety Allergenes Neuroscience Neuroinflammation Inhibitors & Compound Libraries Small Molecules By Organ Pancreatic Cancer
Typ	Inhibitors
Specific against	other
Smiles	C1=CC(=C(C=C1F)O)C2=CC=C(O2)C=C3C(=O)NC(=O)S3
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	900515-16-4'
Similar products	AS-252424
Lieferbar
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	305, 28
Administration	Oral administration 15 minutes before injection of thioglycollate
Animal Models	Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
Cell lines	Raw-264 macrophage
Concentrations	0.01 nM to 0.1 uM
Dosages	10 mg/kg
Formulation	AS-252424 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
IC50	33 nM, 33 nM, 33 nM, 33 nM, 33 nM, 33 nM
In vitro	AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kgamma inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kalpha with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 uM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 uM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 uM. [1] AS252424, 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 AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3]
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 PI3Kgamma-deficient mice. [1]
Incubation Time	5 minutes
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	After 3 hours of starvation in serum-free medium, Raw-264 macrophages are pretreated with AS-252424 or DMSO for 30 minutes and stimulated for 5 minutes with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols.
Solubility (25C)	DMSO 61 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	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.
Chemical Name	(Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2, 4-dione

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