AS2863619 free base

≥99%

CAS编号: 2241300-50-3
分子式: C₁₆H₁₂N₈O
分子量: 332.32
PubChem编号: 139600292

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货号 (SKU)	包装规格	是否现货
A649143-5mg	5mg	期货
A649143-10mg	10mg	期货
A649143-50mg	50mg	期货

查看相关系列

CDK (252) Cell Cycle/DNA Damage (2603) JAK/STAT Signaling (505) STAT (139) Stem Cell/Wnt (1018)

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基本描述

别名	AS2863619 游离碱
规格或纯度	≥99%
英文名称	AS2863619 free base
生化机理	AS2863619 free base 能将抗原特异性效应/记忆 T 细胞转化为 Foxp3 + 调节性 T（T reg）细胞，用于治疗各种免疫性疾病。AS2863619 free base 是一种强效的口服活性细胞周期蛋白依赖性激酶 8 (CDK8)
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	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 IC 50 s 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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. 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 . MCE 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. Form:Solid IC50& Target: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

名称和识别符

IUPAC Name	4-[1-(2-methyl-3H-benzimidazol-5-yl)imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine
INCHI	InChI=1S/C16H12N8O/c1-8-19-10-3-2-9(6-11(10)20-8)24-13-4-5-18-7-12(13)21-16(24)14-15(17)23-25-22-14/h2-7H,1H3,(H2,17,23)(H,19,20)
InChi Key	OORKHRHPVSWORX-UHFFFAOYSA-N
Canonical SMILES	CC1=NC2=C(N1)C=C(C=C2)N3C4=C(C=NC=C4)N=C3C5=NON=C5N
PubChem CID	139600292
分子量	332.32

化学和物理性质

溶解性	DMSO : 250 mg/mL (752.29 mM; Need ultrasonic)
分子量	332.320 g/mol
XLogP3	1.200
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	7
可旋转键计数Rotatable Bond Count	2
精确质量Exact Mass	332.113 Da
单同位素质量Monoisotopic Mass	332.113 Da
拓扑极表面积Topological Polar Surface Area	124.000 Å²
重原子数Heavy Atom Count	25
形式电荷Formal Charge	0
复杂度Complexity	495.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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AS2863619 free base

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基本描述

名称和识别符

化学和物理性质

安全和危险性（GHS）

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

溶液计算器

摩尔浓度计算器

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复溶计算器