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- CAS号：
443797-96-4
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥353.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥689.0 |
| 规格： | 5mg | 产品价格： | ￥794.0 |
| 规格： | 10mg | 产品价格： | ￥1304.0 |
| 规格： | 25mg | 产品价格： | ￥1984.0 |
| 规格： | 50mg | 产品价格： | ￥3184.0 |
| 规格： | 100mg | 产品价格： | ￥4536.0 |
Product Introduction
Bioactivity
| 名称 | JNJ-7706621 |
| 描述 | JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2. |
| 细胞实验 | Cell lines: HeLa,HCT-116,A375,SK-OV-3,MDA-MB-231 and PC-3 cells. Concentrations: 1 nM - 10 μM,dissolved in DMSO. Method: Measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells to determine the ability of JNJ-7706621 to inhibit the proliferation of cell growth.Cells are trypsinized and counted and 3-8 ×103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in 100 μL complete medium in a volume.Cells are incubated for 24 hours at 37 °C in an atmosphere containing 5% CO2.Next,1 μL JNJ-7706621 is added to the wells of the plate.Cells are incubated for another 24 hours.Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL.The plate is incubated for 24 hours at 37 °C in JNJ-7706621 with 14C-thymidine.The contents of the plate are discarded and the plate is washed twice with 200 μL PBS.200 μL of PBS is added to each well.The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate.The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count. |
| 激酶实验 | In vitro kinase assay for CDK1 and Aurora kinases:CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif. |
| 动物实验 | Animal Models: Mouse xenograft model of A375 cellsFormulation & . Dosages: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.100 or 125 mg/kg. Administration: Orally or by intraperitoneal injection |
| 体外活性 | JNJ-7706621（100或125 mg/kg）导致携带A375恶性黑色素瘤人类肿瘤移植瘤模型的小鼠中肿瘤消退. |
| 体内活性 | JNJ-7706621在抑制正常细胞类型（包括MRC-5,HASMC,HUVEC和HMVEC）的生长方面具有几倍的效力,IC50为3.67-5.42 μM。JNJ-7706621对CDK1和2具有高度有效性,IC50为3-9 nM。JNJ-7706621显示对包括HeLa,HCT-116,SK-OV-3,PC3,DU145,A375,MDA-MB-231,MES-SA和MES-SA/Dx5在内的一组人类癌细胞类型的抑制作用 ,IC50为112-514 nM,独立于p53,成视网膜细胞瘤或P-糖蛋白状态。JNJ-7706621也抑制CDK3,4和6,IC50为58-253 nM。JNJ-7706621抑制Aurora-A和B,IC50分别为11和15 nM。JNJ-7706621也抑制VEGF-R2,FGF-R2和GSK3β,IC50为154-254 nM。在HeLa或U937细胞中,JNJ-7706621（0.5-3 μM）延迟从G1期中退出,使细胞停滞在G2-M期,诱导核内复制,激活凋亡并减少集落形成。 |
| 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 | DMSO : 245 mg/mL (621.26 mM), Sonication is recommended. 10% DMSO+90% Saline : < 10 mg/mL (25.36 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (25.36 mM), Solution. |
| 关键字 | JNJ-7706621 | JNJ7706621 | Inhibitor | inhibit | Cyclin dependent kinase | CDK2/CyclinE | CDK2/CyclinA | CDK1/CyclinB | CDK | AuroraKinase | Aurora Kinase | Aurora B | Aurora A | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | 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 | Anti-Pancreatic Cancer Compound Library | Kinase Inhibitor Library | Fluorochemical Library | Anti-Aging Compound Library | Epigenetics Compound Library | Preclinical Compound Library | Membrane Protein-targeted Compound 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 JNJ7706621【443797-96-4】
￥353 - 4536
