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- CAS号：
934353-76-1
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥618.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥293.0 |
| 规格： | 5mg | 产品价格： | ￥551.0 |
| 规格： | 10mg | 产品价格： | ￥928.0 |
| 规格： | 25mg | 产品价格： | ￥1592.0 |
| 规格： | 50mg | 产品价格： | ￥2384.0 |
| 规格： | 100mg | 产品价格： | ￥3304.0 |
Product Introduction
Bioactivity
| 名称 | ENMD-2076 |
| 描述 | ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα. |
| 细胞实验 | The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with ENMD-2076 for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay. The leukemia-derived, nonadherent cell lines are assayed by plating 5 × 103 cells per well in a 96-well plate. The cells are incubated with ENMD-2076 for 48 hours and then survival is assayed using the Alamar Blue reagent. To measure the effect of ENMD-2076 on VEGF- and fibroblast growth factor (FGF)-induced proliferation of human umbilical vein endothelial cell (HUVEC), cells are serum starved for 6 hours, then treated with ENMD-2076 free base, and stimulated with 5 ng/mL bFGF or 25 ng/mL VEGF (R and D Systems) for 72 hours. Cell proliferation is measured using WST-(Only for Reference) |
| 激酶实验 | Kinase assays: Recombinant Aurora A and B kinase enzymes and appropriate PanVera Z'-Lyte kinase assay kits are purchased. Assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values. Potency of ENMD-2076 free base against a select panel of 100 kinase enzymes is determined using the SelectScreen kinase profiling service. ATP concentrations are at the apparent Km for each enzyme or 100 μM if the apparent Km could not be reached. Percent inhibition is determined at an ENMD-2076 free base concentration of 1 μM; for kinases where significant inhibition is noted, IC50 values are determined by generating full 10-point dose–response curves. |
| 体外活性 | 在MDA-MB-231异种移植模型中, ENMD-2076可以抑制形成新血管,同时使形成的血管发生退化.在HT29异种移植模型中,ENMD-2076对Flt3以及VEGFR2 / KDR和FGFR1 / 2的激活持续发挥抑制作用.在H929人浆细胞瘤异种移植物中,口服ENMD-2076（50-200 mg / kg /day）,其中磷酸 - 组蛋白3（pH3）,Ki-67显著降低,裂解的胱天蛋白酶-3显著增加. |
| 体内活性 | ENMD-2076作用于PI3K/AKT通路,下调凋亡抑制蛋白。ENMD-2076能够抑制aurora A和B激酶,且诱导细胞周期停在G2/M 期。在多种作用于血管生成的激酶中（IC50=1.86-120 nM）,ENMD-2076能够发挥作用,比如VEGFR2/KDR 和VEGFR3, FGFR1和FGFR2, 及PDGFRα。在多种人类实体瘤和血癌细胞系中（IC50=0.025 -0.7 μM）,ENMD-2076使细胞停滞在G2/M 期,诱导细胞凋亡 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (8.79 mM), Sonication is recommended. DMSO : 97 mg/mL (258.34 mM), Sonication is recommended. H2O : 1 mg/mL (2.66 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | VEGFR3/FLT4 | VEGFR | Vascular endothelial growth factor receptor | Src | RET | Platelet-derived growth factor receptor | PDGFR | Inhibitor | inhibit | Fms like tyrosine kinase 3 | FLT3 | Fibroblast growth factor receptor | FGFR | ENMD-2076 | ENMD2076 | ENMD 2076 | cRET | Cluster of differentiation antigen 135 | CD135 | AuroraKinase | Aurora Kinase | Aurora A | Apoptosis |
| 相关产品 | Formamide | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Ferulic Acid | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 ENMD-2076【934353-76-1】
￥293 - 3304
