5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷
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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CAS:900515-16-4别名：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;AS252424;5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮2MG英文名：5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
- 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.
