5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione

5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Basic information
Product Name:5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
Synonyms:5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione;AS-252424;(E)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)Methylene)thiazolidine-2,4-dione;(Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione;AS 252424 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione;AS-252424;AS 252424;(5Z)-5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione;AS-252424cas
CAS:900515-16-4
MF:C14H8FNO4S
MW:305.28
EINECS:
Product Categories:Inhibitors;Akt;mTOR;PI3K;Phosphoinositide 3-kinase PI3-kinase p110γ inhibitor.;A phosphoinositide 3-kinase PI3-kinase p110γ inhibitor.
Mol File:900515-16-4.mol
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Structure
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Chemical Properties
Melting point >235oC (dec.)
density 1.559±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: >20mg/mL
pka7.20±0.20(Predicted)
form solid
color yellow
Safety Information
WGK Germany 3
MSDS Information
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Usage And Synthesis
UsesAS-252424 is a novel, potent, and selective phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor. It is also an inhibitor of Casein kinase and PI3K p110α.
Biological Activityas-252424 is a potent, selective and novel small-molecule pi3kγ inhibitor (ic50= 30 nm)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in thp-1 (human monocytic cell line), as-252424 inhibited the phosphorylation of pkb/akt due to mcp1 binding to the gpcr receptor ccr2 at lowest ic50 values of 0.4 μm. in primary monocytes and monocytic wild-type cell line thp-1, as-252424 inhibited mcp-1-mediated chemotaxis in a concentration-dependent manner (ic50 value= 52 μm and 53 μm, respectively). [1] in capan 1 and hpaf (pancreatic cancer cell lines), as52424 specifically inhibited the cell proliferation. [2]in a mouse model of thioglycollate-induced peritonitis, oral administration of as-252424 at 10 mg/kg led to moderate reduction of neutrophil recruitment (35% ±14%). [1]
Biochem/physiol ActionsAS-252424 is a potent and selective phosphoinositide 3-kinase PI3Kγ inhibitor with IC50 = 30 nM in a mouse model.
references1. pomel v, klicic j, covini d et al. furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. j med chem. 2006 jun 29;49(13):3857-71.2. edling ce, selvaggi f, buus r et al. key role of phosphoinositide 3-kinase class ib in pancreatic cancer. clin cancer res. 2010 oct 15;16(20):4928-37.
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Preparation Products And Raw materials
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- Dihydroxybenzoic acid LY 294002 HYDROCHLORIDE Dihydrocaffeic acid CAL-101 IPI 145 Pictilisib GSK2636771 AS 604850 2-HYDROXYACETOPHENONE 2'-Hydroxyacetophenone

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