AS2863619 free base|cas:2241300-50-3|西域试剂

AS2863619 free base,99.68%

产品编号：Bellancom-126675| CAS NO：2241300-50-3| 分子式：C₁₆H₁₂N₈O| 分子量：332.32

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货号	价格	库存与货期
Bellancom-126675	￥3100.00	杭州北京（现货）
Bellancom-126675	￥4900.00	杭州北京（现货）
Bellancom-126675	￥14700.00	杭州北京（现货）

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AS2863619 free base

产品介绍

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 (T_reg) 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。

生物活性

AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3⁺ regulatory T (T_reg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC₅₀s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (752.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0091 mL	15.0457 mL	30.0915 mL
5 mM	0.6018 mL	3.0091 mL	6.0183 mL
10 mM	0.3009 mL	1.5046 mL	3.0091 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。