AS-252424は、PI3Kγの新しくて、強力で、選択的な阻害剤で、IC50 が 33 nMです。

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AS-252424 化学構造
分子量: 305.28



Quality Control & MSDS




情報 AS-252424は、PI3Kγの新しくて、強力で、選択的な阻害剤で、IC50 が 33 nMです。
目標 PI3Kγ CK2 (casein kinase 2) PI3Kα
IC50 33 nM 20 nM 935 nM [1]
In vitro試験 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. [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試験 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. [1]

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

In vitro PI3Kγ 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.

細胞アッセイ: [1]

細胞系 Raw-264 macrophage
濃度 0.01 nM to 0.1 μM
処理時間 5 minutes
方法 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.

動物実験: [1]

動物モデル Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
製剤 AS-252424 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
投薬量 10 mg/kg
管理 Oral administration 15 minutes before injection of thioglycollate



Download AS-252424 SDF
分子量 305.28


CAS No. 900515-16-4
別名 N/A
溶解度 (25°C)
  • DMSO 61 mg/mL
  • 水 <1 mg/mL
  • エタノール <1 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 (Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione


カスタマーレビュー (1)

Click to enlarge
Source Dr. Zhang of Tianjin Medical University. AS-252424 purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results AS-252424 treatment resulted in a reduction of AKT phosphorylation.

製品表彰状 (3)

  • Phosphoinositide 3 kinase inhibition restores neutrophil accuracy in the elderly: towards targeted treatments for immunesenescence. [Sapey E, et al. Blood 2014;123(2):239-51]

    PubMed: 24191150
  • Pharmacological profiling of phosphoinositide-3-kinase inhibitors as mitigators of ionizing radiation-induced cell death. [Lazo JS, et al. J Pharmacol Exp Ther 2013;347(3):669-80]

    PubMed: 24068833
  • Selective CDK9 inhibition overcomes TRAIL resistance by concomitant suppression of cFlip and Mcl-1. [Lemke J ,et al. Cell Death Differ 2013;10.1038/cdd.2013.179]

    PubMed: 24362439



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


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