900515-16-4
中文名稱
5-[[5-(4-氟-2-羥基苯基)-2-呋喃基]亞甲基]-2,4-噻唑烷二酮
英文名稱
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
CAS
900515-16-4
分子式
C14H8FNO4S
分子量
305.28
MOL 文件
900515-16-4.mol
更新日期
2024/12/22 16:36:06
900515-16-4 結(jié)構(gòu)式
基本信息
中文別名
化合物AS-252424PI3KΓ抑制劑(AS-252424)
5-[[5-(4-氟-2-羥基苯基)-2-呋喃基]亞甲基]-2,4-噻唑烷二酮
5-[[5-(4-氟-2-羥基苯基)-2-呋喃基]亞甲基]-2,4-噻唑烷二酮 2MG
英文別名
CS-182AS-252424
AS-252424cas
AS-252424
AS 252424
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
(Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
(E)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)Methylene)thiazolidine-2,4-dione
(5Z)-5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 5-[[5-(4-fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-, (5Z)-
AS 252424 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
常見問題列表
生物活性
AS-252424是一種新型，有效的PI3Kγ抑制劑，IC50為30 nM，作用于PI3Kγ比作用于PI3Kα選擇性高30倍，對PI3Kδ/β具有低的抑制活性。體外研究
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.體內(nèi)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.靶點
|
PI3Kα 935 nM (IC 50 ) |
PI3Kγ 30 nM (IC 50 ) |
PI3Kδ 20 μM (IC 50 ) |
PI3Kβ 20 μM (IC 50 ) |