AS2863619 free base

AS2863619 free base

中文名称AS2863619 free base
中文同义词化合物 T10382;化合物 AS2863619 FREE BASE
英文名称AS2863619 free base
英文同义词AS2863619 free base;1,2,5-Oxadiazol-3-amine, 4-[1-(2-methyl-1H-benzimidazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl]-;AS-2863619 free base,AS2863619 free base
CAS号2241300-50-3
分子式C16H12N8O
分子量332.32
EINECS号
相关类别
Mol文件2241300-50-3.mol
结构式AS2863619 free base 结构式

AS2863619 free base 性质

沸点755.8±70.0 °C(Predicted)
密度1.75±0.1 g/cm3(Predicted)
储存条件Store at -20°C
溶解度二甲基亚砜:250 mg/ml(752.29 mM)
形态固体
酸度系数(pKa)10.44±0.10(Predicted)
颜色白色至米白色

AS2863619 free base 用途与合成方法

AS2863619 free base 可以将抗原特异性效应子/记忆 T 细胞转换为 Foxp3+ 调节性 T (Treg) 细胞,以研究各种免疫疾病。AS2863619 free base 是一种有效的口服的细胞周期蛋白依赖性激酶 8 (CDK8) 和 CDK19 抑制剂,IC50 分别为 0.61 nM 和 4.28 nM。AS2863619 free base 抑制 CDK8/19 可增强 STAT5 的激活,从而激活 Foxp3 基因。

CDK8

0.61 nM (IC 50 )

CDK19

4.28 nM (IC 50 )

GSK3α

76.67 nM (IC 50 )

GSK3β

63.06 nM (IC 50 )

STAT5

AS2863619 (1 μM; 22 hours; mouse CD4 + T cells) treatment suppresses serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.

Western Blot Analysis

Cell Line: Mouse CD4 + T cells
Concentration: 1 μM
Incubation Time: 22 hours
Result: Suppressed serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.

AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ + (IFN-γ + ) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. T reg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1 + Foxp3 + T cells are specifically increased in DNFB sensitized AS2863619-treated mice.

Animal Model: Mice with DNFB-induced contact skin hypersensitivity
Dosage: 30 mg/kg
Administration: Oral administration; daily; for 2 weeks
Result: The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ + (IFN-γ + ) cells.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-126675AS2863619 free base1 mg1409元
2024/08/19HY-126675AS2863619 free base
AS2863619 free base
2241300-50-35mg3100元

AS2863619 free base 上下游产品信息

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