Name: AS-252424
Price: 145.00 USD

- Overview
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    Background
    
    AS-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]
    
    1. 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.
- Properties
  - Alternative Name
    
    (5Z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione
    
    CAS Number
    
    900515-16-4
    
    Molecular Formula
    
    C14H8FNO4S
    
    Molecular Weight
    
    305.28
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥30.5 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AS-252424

AS-252424

Background

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