计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer
In Vitro
VVD-118313 (compound 5a; 0.01-10 μM; 3 h; primary human PBMCs) inhibits JAK1 by engagement of C817 and JAK2 by engagement of C838. VVD-118313 inhibits cysteine reactivity in a dose-dependent manner. VVD-118313 (2 µM, 2h) blocks IFNα-simulated STAT1 and IL-6-stimulated STAT3 phosphorylation in WT- or C810A-JAK1-expressing 22Rv1 cells. VVD-118313 also blocks the constitutive phosphorylation of WT- and C810A-JAK1. VVD-118313 (0.01-10 μM) selectively inhibits JAK1 signaling in primary human immune cells. VVD-118313 inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, and IL-2-pSTAT5 pathways in human PBMCs in a dose-dependent manner. VVD-118313 (0.1-0.4 μM; 24 h) inhibits T-cell activation induction. VVD-118313 inhibits the activation of human T cells co-stimulated with αCD3/αCD28 by a reduction in the proportion of CD25 + T cells. VVD-118313 blocks the secretion of the Th1-polarizing cytokine IFNγ and increases the production of IL-2. VVD-118313 (0.1-0.5 μM; 2 h) inhibits on the production of pro-inflammatory cytokines and chemokines. VVD-118313 suppresses the induction of several pro-inflammatory chemokines, including CCL2/MCP-1, CXCL10/IP-10, and CCL4/MIP-1β. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: 22Rv1 cells Concentration: 0.01, 0.1, and 1 μM Incubation Time: 2 hours Result: Showed labeling of recombinant WT-JAK1 and C810A-JAK1, but not C817A-JAK1. Western Blot AnalysisCell Line: 22Rv1 cells Concentration: 2 µM Incubation Time: 2 hours Result: Inhibited WT- and C810A-JAK1 phosphorylation with even greater potency than STAT1/STAT3 phosphorylation.
In Vivo
VVD-118313 (compound 5a; 25-50 mg/kg; i.h.; once) inhibits JAK1 signaling in TYK2 knockout mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: TYK2 knockout mice Dosage: 25 and 50 mg/kg Administration: Subcutaneous injection; once Result: Revealed 75% engagement of JAK1_C816 at 25 and 50 mg/kg, while other JAK1 cysteines were unaffected in reactivity.
Form:Solid
IC50& Target:JAK1
规格
规格或纯度
≥99%
英文名称
VVD-118313
生化机理
VVD-118313（化合物 5a）是一种强效的选择性 JAK1 抑制剂。VVD-118313 以异构半胱氨酸为靶点，阻断 JAK1 依赖性反式磷酸化和细胞因子信号转导。VVD-118313 可用于癌症研究。
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(N1CCC[C@H](C1)C2=CC(Cl)=C(C=C2)Cl)C#C[C@]3(CCN(S(=O)(C)=O)C3)[H]
分子量
429.36
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (232.90 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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