中文名称:

5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮

中文同义词:

5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮 2MG;5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮;PI3KΓ抑制剂(AS-252424);化合物AS-252424

英文名称:

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

英文同义词:

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;CS-182

CAS号:

900515-16-4

分子式:

C14H8FNO4S

分子量:

305.28

EINECS号:

相关类别:

信号转导通路激酶抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors;Akt;mTOR;PI3K;Phosphoinositide 3-kinase PI3-kinase p110γ inhibitor.;A phosphoinositide 3-kinase PI3-kinase p110γ inhibitor.

Mol文件:

900515-16-4.mol

储存条件 

2-8°C

溶解度 

DMSO: >20mg/mL

形态

solid

颜色

yellow

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 doesnt 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 )

PI3Kα 935 nM (IC 50 )

PI3Kγ 30 nM (IC 50 )

WGK Germany 

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