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    AS-252424
    AS-252424

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0130
    CAS #: 900515-16-4Purity ≥98%

    Description: AS-252424 is a novel, potent, orally bioactive and selective PI3Kγ inhibitor with potential anticancer activity. It inhibits PI3Kγ with an IC50 of 30 nM in a cell-free assay and showed 30-fold selectivity for PI3Kγ over PI3Kα, as well as low inhibitory activity against PI3Kδ/β. In Capan 1 and HPAF (pancreatic cancer cell lines), AS52424 specifically inhibited the cell proliferation.

    References:J Med Chem. 2006 Jun 29;49(13):3857-71; Clin Cancer Res. 2010 Oct 15;16(20):4928-37.

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    Molecular Weight (MW)

    305.28

    Formula

    C14H8FNO4S

    CAS No.

    900515-16-4

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 61 mg/mL (199.81 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    4% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5mg/mL 

    Other info

    Synonym: AS252424; AS 252424; AS-252424.

    Chemical Name: (Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione

    InChi Key: OYYVWNDMOQPMGE-SDQBBNPISA-N

    InChi Code: InChI=1S/C14H8FNO4S/c15-7-1-3-9(10(17)5-7)11-4-2-8(20-11)6-12-13(18)16-14(19)21-12/h1-6,17H,(H,16,18,19)/b12-6-

    SMILES Code: O=C(NC/1=O)SC1=C/C2=CC=C(C3=CC=C(F)C=C3O)O2


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    In Vitro

    Kinase Assay: Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[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.

     

    Cell Assay: 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.  

    AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kα 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 μM 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 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes.

    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 PI3Kγ-deficient mice.

    Animal model

    Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model

    Formulation & Dosage

    Dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.; 10 mg/kg; oral administration。

    References

    [1] Pomel V, et al, J Med Chem, 2006, 49(13), 3857-3871.; [2] Edling CE, et al, Clin Cancer Res, 2010, 16(20), 4928-4937.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AS-252424

    Clin Cancer Res, 2010, 16(20), 4928-4937.
    AS-252424


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