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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) |
|---|
GSK1070916, 丝氨酸/苏氨酸蛋白激酶 Aurora-C 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
GSK1070916是可逆的ATP竞争性Aurora B和C抑制剂，IC50分别为3.5 nM和6.5 nM。而对于Aurora A-TPX2复合物的IC50则为490 nM。
Information
GSK1070916 is a reversible and ATP-competitive inhibitor ofAurora B/CwithIC50of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
In vitro
GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis. In another study, it is also reported high chromosome number associated with resistance to the inhibition of Aurora B and C suggests cells with a mechanism to bypass the high ploidy checkpoint are resistant to GSK1070916.
In vivo
GSK1070916 (25, 50, or 100 mg/kg) shows dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models.
Cell Data
cell lines：
Concentrations：0-15 mM
Incubation Time：6-7 days
Powder Purity:≥97%
规格
英文别名
3-(4-(4-(2-(3-((dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea
规格或纯度
Moligand™, 10mM in DMSO
英文名称
GSK1070916
生化机理
GSK1070916 是一种 Aurora B/C 的可逆 ATP 竞争性抑制剂，IC50 为 3.5 nM/6.5 nM。它对密切相关的 Aurora A-TPX2 复合物的选择性大于 100 倍。第 1 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
丝氨酸/苏氨酸蛋白激酶 Aurora-C 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC=CC(=C5)CN(C)C
分子量
507.63
Reaxy-Rn
15498355
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15498355&ln=
技术文档
高级数据
产品属性
| ALogP | 3.9 |
|---|
关联靶点（人）
DDR1
Tchem
上皮盘状结构域受体 1(Epithelial discoidin domain-containing receptor 1)
(1 活性数据)
AURKA
Tchem
极光激酶A(Aurora kinase A)
(6 活性数据)
AURKB
Tchem
极光激酶B(Aurora kinase B)
(5 活性数据)
AURKC
Tchem
极光激酶C(Aurora kinase C)
(5 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 85 mg/mL (197.86 mM); Ethanol: 85 mg/mL (197.86 mM); Water: Insoluble;
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
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