生物活性 体外研究 体内研究 靶点 5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮 试剂级价格
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5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮

5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮,900515-16-4,结构式
5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮
  • CAS号:900515-16-4
  • 英文名:5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
  • 中文名:5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮
  • CBNumber:CB82093286
  • 分子式:C14H8FNO4S
  • 分子量:305.28
  • MOL File:900515-16-4.mol
5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮化学性质
  • 熔点 :>235oC (dec.)
  • 密度 :1.559±0.06 g/cm3(Predicted)
  • 储存条件 :2-8°C
  • 溶解度 :DMSO: >20mg/mL
  • 酸度系数(pKa) :7.20±0.20(Predicted)
  • 形态 :solid
  • 颜色 :yellow
安全信息
  • WGK Germany :3

5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮性质、用途与生产工艺

  • 生物活性 AS-252424是一种新型,有效的PI3Kγ抑制剂,IC50为30 nM,作用于PI3Kγ比作用于PI3Kα选择性高30倍,对PI3Kδ/β具有低的抑制活性。
  • 体外研究 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.
  • 体内研究 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.
  • 靶点

    PI3Kα

    935 nM (IC 50 )

    PI3Kγ

    30 nM (IC 50 )

    PI3Kδ

    20 μM (IC 50 )

    PI3Kβ

    20 μM (IC 50 )

5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮上下游产品信息
上游原料
下游产品
5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮 试剂级价格
  • 更新日期:2024/11/08
  • 产品编号:HY-13532
  • 产品名称:AS-252424
  • CAS编号:
  • 包装:1 mg
  • 价格:350元
  • 更新日期:2024/11/08
  • 产品编号:HY-13532
  • 产品名称:5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮 AS-252424
  • CAS编号:900515-16-4
  • 包装:5mg
  • 价格:770元
5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮生产厂家
  • 公司名称:SIGMA
  • 联系电话:--
  • 电子邮件:
  • 国家:瑞士
  • 产品数:6896
  • 优势度:91
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