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-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
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

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

5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 用途与合成方法

AS-604850 是一种有效的,具有选择性的和 ATP 竞争性的 PI3Kγ 抑制剂,IC50 值为 0.25 μM,Ki 值为 0.18 μM。AS-604850 是 PI3Kγ 的同工型选择性抑制剂,对 PI3Kγ 的选择性是 PI3Kδ/β 的 30 倍以上,是 PI3Kα 的 18 倍以上。

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.

安全信息

危险品标志Xi
危险类别码43
安全说明36/37
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-13531AS-6048501 mg190元
2024/01/25HY-135315-[(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
648449-76-75mg650元

5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮 上下游产品信息

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苯并噻吩 YO01027 二苯并噻吩 PD173074 司美替尼 尼达尼布 4-十二烷基-N-1,3,4-噻二唑-2-基苯磺酰胺 OSU-03012(AR-12) AT9283
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