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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) |
|---|
Alisertib (MLN8237), 丝氨酸/苏氨酸蛋白激酶 Aurora-A 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
Alisertib (MLN8237)是Aurora A选择性抑制剂，IC50为1.2 nM，比对Aurora B的抑制性高200倍。
Information
Alisertib (MLN8237) is a selectiveAurora Ainhibitor withIC50of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest,apoptosisandautophagy. Phase 3.
In vitro
MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib. MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment.
In vivo
MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：24, 48, and 72 hours
Powder Purity:≥99%
规格
英文别名
Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Alisertib (MLN8237)
生化机理
Alisertib （MLN8237）是一种选择性 Aurora A 抑制剂，在无细胞试验中的 IC50 为 1.2 nM。Alisertib 可诱导细胞周期停滞、细胞凋亡和自噬。第 3 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-A 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC
分子量
518.94
Reaxy-Rn
18350078
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18350078&ln=
技术文档
高级数据
产品属性
| ALogP | 5 |
|---|
关联靶点（人）
GABRA1
Tclin
γ-氨基丁酸受体亚基α-1(Gamma-aminobutyric acid receptor subunit alpha-1)
(1 活性数据)
DNAJA1
Tchem
DnaJ 同源亚家族 A 成员 1(DnaJ homolog subfamily A member 1)
(1 活性数据)
MCM4
Tchem
DNA复制许可因子MCM4(DNA replication licensing factor MCM4)
(1 活性数据)
AURKA
Tchem
极光激酶A(Aurora kinase A)
(15 活性数据)
AURKB
Tchem
极光激酶B(Aurora kinase B)
(2 活性数据)
ACAD10
Tchem
酰基辅酶 A 脱氢酶家族成员 10(Acyl-CoA dehydrogenase family member 10)
(1 活性数据)
GNAI2
Tchem
鸟嘌呤核苷酸结合蛋白 G(i) 亚基 α-2(Guanine nucleotide-binding protein G(i) subunit alpha-2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 62 mg/mL warmed with 50ºC Water: bath (198.48 mM); Water: Insoluble; Ethanol: 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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