计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
ENMD-2076, 巨噬细胞集落刺激因子受体抑制剂
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
Information
ENMD-2076 has selective activity againstAurora AandFlt3withIC50of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide
In vitro
ENMD-2076 indicates activity against multiple kinases involved in angiogenesis, including FLT3, RET, FLT4/VEGFR3, SRC, NTRK1, CSF1R/FMS, LCK, VEGFR2/KDR, FGFR1/2, and PDGFRα with IC50 from 1.86-120 nM. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. ENMD-2076 induces regression or complete inhibition of tumor growth in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines. ENMD-2076 is the L (+) tartrate salt of ENMD-981693. ENMD-2076 shows significant cytotoxicity against myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells with IC50 from 2.99 to 7.06 μM, which induces apoptosis. ENMD-2076 indicates low cytotoxicity to haematopoietic progenitors. ENMD-2076 inhibits the phosphoinositide 3-kinase/Akt pathway and downregulates survivin and X-linked inhibitor of apoptosis. ENMD-2076 also inhibits aurora A and B kinases, and induces G2/M cell cycle arrest.
In vivo
ENMD-2076 has sustained inhibitory effects on the activation of Flt3 as well as VEGFR2/KDR and FGFR1/2 in HT29 xenograft model. ENMD-2076 could prevent the formation of new blood vessels and regress formed vessels in MDA-MB-231 xenograft model. Oral treatment with ENMD-2076 (50, 100, 200 mg/kg per day) inhibits the tumour growth in H929 human plasmacytoma xenografts, with significant reduction in phospho-Histone 3 (pH3), Ki-67, and angiogenesis, and also a significant increase in cleaved caspase-3.
Cell Data
cell lines：
Concentrations：0.3 nM - 125 μM
Incubation Time：48 or 96 hours
Powder Purity:≥99%
规格
英文别名
(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine
规格或纯度
Moligand™, 10mM in DMSO
英文名称
ENMD-2076
生化机理
ENMD-2076对Aurora A和Flt3具有选择性活性，IC50分别为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα的作用较弱。ENMD-2076能抑制多种人类实体瘤和造血癌细胞株的生长，IC50为0.025至0.7 μM，并能诱导细胞凋亡和G2/M期停滞。第 2 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
巨噬细胞集落刺激因子受体抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CC(=NN1)NC2=CC(=NC(=N2)/C=C/C3=CC=CC=C3)N4CCN(CC4)C
分子量
375.47
Reaxy-Rn
24925441
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24925441&ln=
技术文档
高级数据
产品属性
| ALogP | 3.7 |
|---|
关联靶点（人）
PTK2
Tclin
粘着斑激酶1(Focal adhesion kinase 1)
(1 活性数据)
CSF1R
Tclin
巨噬细胞集落刺激因子 1 受体(Macrophage colony-stimulating factor 1 receptor)
(1 活性数据)
RET
Tclin
原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret)
(1 活性数据)
SRPRA
Tchem
信号识别颗粒受体亚基α(Signal recognition particle receptor subunit alpha)
(1 活性数据)
SRC
Tclin
原癌基因酪氨酸蛋白激酶Src(Proto-oncogene tyrosine-protein kinase Src)
(3 活性数据)
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(5 活性数据)
PDGFRA
Tclin
血小板衍生生长因子受体α(Platelet-derived growth factor receptor alpha)
(2 活性数据)
AURKA
Tchem
极光激酶A(Aurora kinase A)
(11 活性数据)
KDR
Tclin
血管内皮生长因子受体 2(Vascular endothelial growth factor receptor 2)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 50 mg/mL (200.59 mM); Ethanol: 5 mg/mL (20.05 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:
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 |
|---|---|---|
 L2214622 |
分析证书 | E408042 |
溶液计算器
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