- ￥134 - 1800
- TargetMol
- T2680
- 2026年07月07日
2 年钻石会员
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- CAS号：
1185763-69-2
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥266.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥134.0 |
| 规格： | 5mg | 产品价格： | ￥334.0 |
| 规格： | 10mg | 产品价格： | ￥474.0 |
| 规格： | 25mg | 产品价格： | ￥904.0 |
| 规格： | 50mg | 产品价格： | ￥1280.0 |
| 规格： | 100mg | 产品价格： | ￥1800.0 |
Product Introduction
Bioactivity
| 名称 | NVP-BVU972 |
| 描述 | NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM. |
| 细胞实验 | BaF3 cells containing TPR-MET or various mutants thereof are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental BaF3 cells the medium is additionally supplemented with 10 ng/mL interleukin-3 (IL-3). For proliferation assays, BaF3 cells are seeded on 96-well-plates in triplicates at 104 cells per well and incubated with various concentrations of NVP-BVU972 for 72 hours followed by quantification of viable cells using a resazurin sodium salt dye reduction readout. IC50 values are determined with the XLFit Excel Add-In using a 4-parameter dose response model.(Only for Reference) |
| 激酶实验 | TR-FRET biochemical assay with MET wild type and mutants: Enzyme activity is measured in a time resolved fluorescence resonance energy transfer (TR-FRET) assay, detecting tyrosine phosphorylation with a Eu-labelled anti-phospho-tyrosine antibody (fluorescence donor) and Allophycocyanin conjugated to Streptavidin (fluorescence acceptor) which binds to a biotin on the substrate peptide. For each variant, Km concentrations for ATP are determined in the absence of NVP-BVU972, and the ATP concentration in the kinase reaction is set to Km (4 μM for MET wt, 1 μM for MET Y1230H and MET F1200I). NVP-BVU972 is dissolved and diluted in DMSO and assayed in quadruplicate. Kinase reactions are carried out in 50 mM Tris-HCl pH 7.5, 8 mM MgCl2, 4 mM MnCl2, 0.05 % Tween 20, 0.05% bovine serum albumin, 0.1 mM EDTA, 1 mM DTT, 0.1 mM Na3VO4, in white 1536 well plates at room temperature. NVP-BVU972 and enzyme are incubated in a volume of 2 μL for 20 min, followed by the addition of 1 μL ATP and 1 μL biotinylated peptide substrate (PTK1) to final concentrations of Km and 1 μM, respectively. Enzyme concentrations in the reactions are 5 nM for MET wt, and 4 nM for the F1200I and Y1230H variants. After 90 min, reactions are stopped by addition of 1 μL stop/detection solution to reach final concentrations of 10 mM EDTA, 3.5 nM Eu-labelled antiphospho-tyrosine antibody PY20, and 10 nM Streptavidin Allophycocyanin. Time resolved fluorescence resonance energy transfer is measured in an Envision plate reader (excitation 320 nm, emission 615 nm and 665 nm). |
| 体内活性 | NVP-BVU972有效抑制MET基因扩散的细胞系GTL-16,MKN-45和EBC-1的生长,IC50分别为66,82和32 nM。NVP-BVU972有效抑制MET激酶,而对其他激酶（包括最密切相关的激酶）RON抑制作用很低,IC50>1000 nM。NVP-BVU972抑制GTL-16细胞中组成型MET磷酸化,抑制A549细胞中HGF刺激的MET磷酸化,IC50分别为7.3和 22 nM。NVP-BVU972作用于表达野生型TPR-MET的BaF3细胞,剂量依赖性降低TPR-MET磷酸化。 |
| 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 : 45 mg/mL (132.21 mM), Sonication is recommended. Ethanol : 63 mg/mL (185.09 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.88 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | phosphorylation | NVP-BVU-972 | NVP-BVU972 | NVPBVU972 | NVP-BVU 972 | NVP BVU972 | MET resistance mutations | Met | Inhibitor | inhibit | HGFR | c-Met/HGFR | cMet/HGFR | c-Met | cMet | cancer | BaF3 TPR-MET | BaF3 | anti-proliferation |
| 相关产品 | Cabozantinib S-malate | Crizotinib | Tepotinib | (Z)-Semaxinib | Afatinib | Afatinib Dimaleate | Capmatinib | Decanoic Acid | L-Ascorbic acid 2-phosphate trisodium | 7-Methoxy-1-tetralone | Bacitracin Zinc | (S)-Afatinib |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Pancreatic Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | Reprogramming Compound Library |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验该产品被引用文献
官网有文献
相关实验
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。
技术资料暂无技术资料 索取技术资料
文献支持
化合物 NVP-BVU972【1185763-69-2】
￥134 - 1800
