5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮
| 中文名称 | 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 |
|---|---|
| 中文同义词 | 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮;5-(2,2-二氟-苯唑[1,3]二氧-5-基亚甲基)-噻唑烷-2,4-二酮;AS-604850游离态;5-((2,2-二氟苯并[D][1,3]二氧杂环戊烯-5-基)亚甲基)噻唑烷-2,4-二酮;AS-604850,ATP竞争性PI3KΓ抑制剂;化合物 AS604850;AS-604850,ATP-COMPETITIVE PI3KGAMMA抑制剂;化合物AS604850,10 MM DMSO 溶液 |
| 英文名称 | AS 604850 |
| 英文同义词 | AS 604850;PI3Kγ inhibitor, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione;PI 3-Kinase Inhibitor (AS604850) B-0302;(Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione;5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione;AS-604850;AS 604850;PI 3-Kγ Inhibitor II;5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione |
| CAS号 | 648449-76-7 |
| 分子式 | C11H5F2NO4S |
| 分子量 | 285.22 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;Akt;mTOR;PI3K;Inhibitors |
| Mol文件 | 648449-76-7.mol |
| 结构式 | ![5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 结构式](CAS/GIF/648449-76-7.gif) |
5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 性质
| 密度 | 1.71 |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：>10mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 7.07±0.20(Predicted) |
| 颜色 | 米白色 |
| InChI | 1S/C11H5F2NO4S/c12-11(13)17-6-2-1-5(3-7(6)18-11)4-8-9(15)14-10(16)19-8/h1-4H,(H,14,15,16)/b8-4- |
| InChIKey | SRLVNYDXMUGOFI-YWEYNIOJSA-N |
| SMILES | FC1(F)Oc2ccc(cc2O1)\C=C3/SC(=O)NC3=O |
|
PI3Kγ 0.25 μM (IC 50 ) |
PI3Kγ 0.18 μM (Ki) |
PI3Kα 4.5 μM (IC 50 ) |
AS-604850 inhibits C5a-mediated PKB phosphorylation with an
IC
50
of 10 μM in RAW264 mouse macrophages.
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg
+/+
or Pik3cg
–/–
mice.
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg
+/+
mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg
+/+
mice.
Western Blot Analysis
| Cell Line: | Primary monocytes from Pik3cg +/+ mice |
| Concentration: | 0 μM, 1 μM, 3 μM, 10 μM, 30 μM |
| Incubation Time: | 15 minutes |
| Result: | Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice. |
AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment.
| Animal Model: | Balb/C or C3H mice with human recombinant RANTES or thioglycollate |
| Dosage: | 10 mg/kg, 30 mg/kg or 100 mg/kg |
| Administration: | Oral administration; for 4.5 or 4.25 hours |
| Result: | Reduced RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-13531 | 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 AS-604850 | 648449-76-7 | 5mg | 348元 |
| 2026/09/15 | HY-13531 | 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 AS-604850 | 648449-76-7 | 10 mM * 1 mLin DMSO | 382元 |