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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) |
|---|
AZD8330, 双特异性丝裂原活化蛋白激酶激酶 2 抑制剂
有货
概述
AZD8330(ARRY-424704; ARRY-704)是非ATP竞争性MEK 1/2抑制剂，IC50为7 nM。An antineoplastic selective MEK inhibitor
Information
AZD8330 (ARRY704) is a novel, selective, non-ATP competitiveMEK 1/2inhibitor withIC50of 7 nM. Phase 1.
In vitro
AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.
In vivo
In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily.
Cell Data
cell lines：
Concentrations：~10 μM
Incubation Time：1 hour
Powder Purity:≥99%
规格
英文别名
ARRY704 | 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AZD8330
生化机理
AZD8330 (ARRY704) 是一种新型、选择性、非 ATP 竞争性 MEK 1/2 抑制剂，IC50 为 7 nM。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
双特异性丝裂原活化蛋白激酶激酶 2 抑制剂
名称和识别符
EC号
642-441-7
分子类型
小分子
Isomeric SMILES
CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO
分子量
461.23
Reaxy-Rn
14467135
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14467135&ln=
高级数据
产品属性
| ALogP | 2.2 |
|---|
关联靶点（人）
MAP2K2
Tclin
双特异性丝裂原活化蛋白激酶激酶 2(Dual specificity mitogen-activated protein kinase kinase 2)
(1 活性数据)
MAP2K1
Tclin
双特异性丝裂原活化蛋白激酶激酶 1(Dual specificity mitogen-activated protein kinase kinase 1)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 0.01 mg/mL (0.04 mM); Water: Insoluble; Ethanol: Insoluble;
折光率
1.66
安全和危险性（GHS）
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:
技术文档和文章
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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