AS2863619 free base
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- CAS号:
- 2241300-50-3
- 英文名:
- AS2863619 free base
- 英文别名:
- AS2863619 free base;AS-2863619 free base,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]-
- 中文名:
- AS2863619 free base
- 中文别名:
- 化合物 T10382
- CBNumber:
- CB95821250
- 分子式:
- C16H12N8O
- 分子量:
- 332.32
- MOL File:
- 2241300-50-3.mol
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AS2863619 free base化学性质
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沸点:
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755.8±70.0 °C(Predicted)
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密度:
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1.75±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 250 mg/mL (752.29 mM)
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酸度系数(pKa):
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10.44±0.10(Predicted)
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AS2863619 free base性质、用途与生产工艺
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。
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CDK8
0.61 nM (IC
50
)
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CDK19
4.28 nM (IC
50
)
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GSK3α
76.67 nM (IC
50
)
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GSK3β
63.06 nM (IC
50
)
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STAT5
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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
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Cell Line:
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Mouse CD4
+
T cells
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Concentration:
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1 μM
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Incubation Time:
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22 hours
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Result:
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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.
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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.
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Animal Model:
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Mice with DNFB-induced contact skin hypersensitivity
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Dosage:
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30 mg/kg
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Administration:
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Oral administration; daily; for 2 weeks
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Result:
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The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ
+
(IFN-γ
+
) cells.
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AS2863619 free base
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-126675 | AS2863619 free base | | 1 mg | 1409元 |
| 2024/04/30 | HY-126675 | AS2863619 free base
AS2863619 free base | 2241300-50-3 | 5mg | 3100元 |
2241300-50-3, AS2863619 free base 相关搜索:
- 化合物 T10382
- 2241300-50-3
- AS-2863619 free base,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]-
- AS2863619 free base