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- TargetMol
- T6609
- 2026年07月07日
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- 详细信息
- 文献和实验
- 技术资料
- CAS号：
1253584-84-7
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥172.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥394.0 |
| 规格： | 5mg | 产品价格： | ￥354.0 |
| 规格： | 10mg | 产品价格： | ￥590.0 |
| 规格： | 25mg | 产品价格： | ￥1240.0 |
| 规格： | 50mg | 产品价格： | ￥1816.0 |
| 规格： | 100mg | 产品价格： | ￥2600.0 |
| 规格： | 200mg | 产品价格： | ￥3656.0 |
Product Introduction
Bioactivity
| 名称 | NMS-E973 |
| 描述 | NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
| 激酶实验 | Hsp90 binding assays: For competition experiments, a protein concentration of 5 nM for Hsp90 and of 200 nM for Trap1 are mixed with 0.5 nmol/L probe (final concentrations). After incubation, the dimethyl sulfoxide (DMSO) compound solution is added to the mixture. The plate is incubated for 18 hours at room temperature and then the fluorescence polarization signal was measured. Data are fitted with the program Dynafit version 3.28.039 or SigmaPlot (SSI) using the mathematical equation for competitive binding of 2 ligands to the receptor. |
| 体外活性 | NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways. [1] |
| 体内活性 | NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. [1] In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90. [2] |
| 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 : 83 mg/mL (182.65 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.26 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | ovary | NMS-E-973 | NMS-E973 | NMSE973 | NMS-E 973 | NMS E973 | Neuroblastoma | Melanoma | Leukemia | Inhibitor | inhibit | Hsp90α | HSP90 | HSP | Heat shock proteins | colon | Carcinoma | cancer | breast | Adenocarcinoma |
| 相关产品 | Mequinol | Isoxazole | 7-Aminocephalosporanic acid | Palmitic acid sodium | Tamoxifen Citrate | Elesclomol | Rifabutin | Palmitic acid | Benzbromarone | Ethoxyquin | Tamoxifen | Adezmapimod |
| 相关库 | Inhibitor Library | CNS-Penetrant Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Exosome Compound Library | Metabolism Compound Library | Highly Selective Inhibitor Library | HIF-1 Signaling Pathway Compound Library | Preclinical Compound Library | Membrane Protein-targeted Compound Library |
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文献和实验网络 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。
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