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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
AZD1480, 酪氨酸蛋白激酶 JAK2 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，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
-80℃储存。特低温运输 。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
AZD1480是ATP竞争性JAK2抑制剂，IC50为0.26 nM，对JAK1抑制性较弱。An inhibitor of JAK2
Information
AZD1480 is a novel ATP-competitiveJAK2inhibitor withIC50of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
In vitro
5μM AZD1480 induces G2/M arrest and cell death by inhibiting Aurora kinases. AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 and STAT3 signaling and downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD1480 blocks cell proliferation and induces apoptosis of myeloma cell lines. AZD1480 effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, and that it is capable of inhibiting STAT3 phosphorylation and tumor growth in a STAT3-dependent manner. AZD1480 inhibits tumor angiogenesis and metastasis in part by affecting the tumor microenvironment.
In vivo
AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. AZD1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model. The Jak2 inhibitor, AZD1480, suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity.
Cell Data
cell lines：
Concentrations：~1 μM
Incubation Time：48 or 24 hours
Powder Purity:≥97%
规格
英文别名
(S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AZD1480
生化机理
AZD1480 是一种新型 ATP 竞争性 JAK2 抑制剂，在无细胞试验中的 IC50 为 0.26 nM，对 JAK3 和 Tyk2 具有选择性，对 JAK1 的选择性较小。第一阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
酪氨酸蛋白激酶 JAK2 抑制剂
名称和识别符
EC号
641-076-0
分子类型
小分子
Isomeric SMILES
CC1=CC(=NN1)NC2=NC(=NC=C2Cl)N[C@@H](C)C3=NC=C(C=N3)F
分子量
348.77
Reaxy-Rn
12890501
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12890501&ln=
技术文档
高级数据
产品属性
| ALogP | 2.4 |
|---|
关联靶点（人）
STAT3
Tchem
信号转导和转录激活因子 3(Signal transducer and activator of transcription 3)
(2 活性数据)
JAK3
Tclin
酪氨酸蛋白激酶JAK3(Tyrosine-protein kinase JAK3)
(1 活性数据)
JAK1
Tclin
酪氨酸蛋白激酶JAK1(Tyrosine-protein kinase JAK1)
(1 活性数据)
STAT5A
Tchem
信号转导和转录激活因子 5A(Signal transducer and activator of transcription 5A)
(2 活性数据)
NTRK1
Tclin
高亲和力神经生长因子受体(High affinity nerve growth factor receptor)
(1 活性数据)
JAK2
Tclin
酪氨酸蛋白激酶JAK2(Tyrosine-protein kinase JAK2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 40 mg/mL (179.92 mM); DMSO: Insoluble; Ethanol: Insoluble;
折光率
1.7
沸点
~575.2 °C at 760 mmHg
熔点
213.39°C
安全和危险性（GHS）
信号词
危险
危险声明
H301: 吞咽会中毒
H361: 怀疑破坏生育力或未出生的孩子
H372: 通过长时间或反复暴露对器官造成损害
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 F2414010 |
分析证书 | A409220 |
技术文档和文章
JAK/STAT 抑制剂
目录： 技术文章
溶液计算器
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