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2241300-50-3

中文名稱 AS2863619 free base
英文名稱 AS2863619 free base
CAS 2241300-50-3
分子式 C16H12N8O
分子量 332.32
MOL 文件 2241300-50-3.mol
更新日期 2023/03/20 15:41:23
2241300-50-3 結(jié)構(gòu)式 2241300-50-3 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10382
英文別名
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]-

物理化學(xué)性質(zhì)

沸點(diǎn)755.8±70.0 °C(Predicted)
密度1.75±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 250 mg/mL (752.29 mM)
酸度系數(shù)(pKa)10.44±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
AS2863619 free base價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-126675AS2863619 free base2241300-50-31 mg1409元
2026/06/05HY-126675AS2863619 free base
AS2863619 free base
2241300-50-35mg3100元
2026/06/05HY-126675AS2863619 free base
AS2863619 free base
2241300-50-310mM * 1mLin DMSO3410元

常見問題列表

生物活性
AS2863619 free base 可以將抗原特異性效應(yīng)子/記憶 T 細(xì)胞轉(zhuǎn)換為 Foxp3+ 調(diào)節(jié)性 T (Treg) 細(xì)胞,以研究各種免疫疾病。AS2863619 free base 是一種有效的口服的細(xì)胞周期蛋白依賴性激酶 8 (CDK8) 和 CDK19 抑制劑,IC50 分別為 0.61 nM 和 4.28 nM。AS2863619 free base 抑制 CDK8/19 可增強(qiáng) STAT5 的激活,從而激活 Foxp3 基因。
靶點(diǎn)

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

體外研究

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.
體內(nèi)研究

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.
"2241300-50-3" 相關(guān)產(chǎn)品信息
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