中文名称: | AS2863619 freebase | ||||
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英文名称: | AS2863619 freebase | ||||
别名: | AS2863619 freebase AS2863619 freebase | ||||
CAS No: | 2241300-50-3 | 分子式: | C16H12N8O | 分子量: | 332.32 |
CAS No: | 2241300-50-3 | ||||
分子式: | C16H12N8O | ||||
分子量: | 332.32 |
基本信息
产品编号:A12275 |
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产品名称:AS2863619 freebase |
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CAS: |
2241300-50-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
332.32 |
-20℃ |
一个月 |
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化学名: |
4-[1-(2-methyl-3H-benzimidazol-5-yl)imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine |
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Solubility (25°C) |
体外 |
DMSO |
200mg/mL (601.83mM; Need ultrasonic) |
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Ethanol |
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Water |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.0091mL |
15.0457mL |
30.0915mL |
5mM |
0.6018mL |
3.0091mL |
6.0183mL |
10mM |
0.3009mL |
1.5046mL |
3.0091mL |
生物活性
产品描述 |
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,抑制CDK8/19可增强STAT5的激活,从而激活Foxp3基因。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。 |
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靶点/IC50 |
CDK8 0.61nM (IC50) |
CDK19 4.28nM (IC50) |
CDK19 4.28nM (IC50) |
GSK3β 63.06nM (IC50) |
体外研究 |
AS2863619 (1μM; 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: |
Mouse CD4+ T cells |
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Concentration: |
1μM |
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Incubation Time: |
22 hours |
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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. |
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体内研究 |
AS2863619 (30mg/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. Treg 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: |
Mice with DNFB-induced contact skin hypersensitivity |
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Dosage: |
30mg/kg |
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Administration: |
Oral administration; daily; for 2 weeks |
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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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )