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- 2026年07月07日
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- CAS号：
915385-81-8
- 规格：
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥206.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥470.0 |
| 规格： | 2mg | 产品价格： | ￥290.0 |
| 规格： | 5mg | 产品价格： | ￥431.0 |
| 规格： | 10mg | 产品价格： | ￥767.0 |
| 规格： | 25mg | 产品价格： | ￥1416.0 |
| 规格： | 50mg | 产品价格： | ￥2376.0 |
| 规格： | 100mg | 产品价格： | ￥4120.0 |
Product Introduction
Bioactivity
| 名称 | Opaganib |
| 描述 | Opaganib (ABC294640) is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM). |
| 细胞实验 | To determine the effects of the test compounds on proliferation, cells are plated into 96-well microtiter plates and allowed to attach for 24 h. Varying concentrations of ABC294640 are added to individual wells and the cells are incubated for an additional 72 h. At the end of this period, the number of viable cells is determined by use of the sulforhodamine-binding assay. The percentage of cells killed is calculated as the percentage decrease in sulforhodamine-binding compared with control cultures. Regression analyses of inhibition curves are performed by use of GraphPad Prism.(Only for Reference) |
| 激酶实验 | Sphingosine Kinase Assays: The IC50 values for ABC294640 and DMS are determined by a newly developed HPLC-based SK activity assay. In brief, the test compounds are incubated with recombinant SK1 or SK2 and NBD-Sph in the isozyme-selective assay buffers detailed below with 1 mg/ml fatty acid-free bovine serum albumin, 100 μM ATP, and 400 μM MgCl2. The product, i.e., NBD-S1P, is separated from NBD-Sph by HPLC as follows: Waters 2795 HPLC system with a Waters 2495 fluorescence detector, C8 Chromolith RP-8e column (100 × 4.6 mm), 1 ml/min mobile phase (acetonitrile/20 mM sodium phosphate buffer, pH2.5, at 45:55). Fluorescence is monitored with excitation at 465 nm and emission at 531 nm. The ratio of NBD-S1P/(NBD-Sph + NBD-S1P) is used as a measure of SK activity. SK-isozyme selective assay buffers each contained 20 mM Tris, pH7.4, 5 mM EDTA, 5 mM EGTA, 3 mM β-mercaptoethanol, 5% glycerol, 1× protease inhibitors and 1× phosphatase inhibitors. For the SK1 assay buffer, 0.25% (final) Triton X-100 is added; and for the SK2 buffer, 1 M (final) KCl is added. Assays are run for 2 h at room temperature, and then a 1.5 volume of methanol is added to terminate the kinase reaction. After 10 min, the samples are centrifuged at 20,000 g to pellet the precipitated protein, and the supernatants are analyzed by HPLC. In experiments to determine the Ki for inhibition of SK2 by ABC294640, the ADP Quest assay system is used to measure kinase activity in the presence of varying concentrations of sphingosine and ABC294640. To determine the effects of ABC294640 on cellular SK activity, near-confluent MDA-MB-231 cells are serum-starved overnight, and then treated with varying concentrations of ABC294640. The cells are then incubated with [3H]sphingosine at a final concentration of 1 μM. The cells take up the exogenous sphingosine, which is converted to S1P via SK activity, and [3H]S1P is separated from [3H]sphingosine by extraction and quantified by scintillation counting. |
| 体外活性 | ABC294640 markedly alters the ratio of ceramide/S1P consistent with inhibition of SK activity in MDA-MB-231 cells. ABC294640 inhibits tumor cell proliferation with IC50 values ranging from approximately 6 to 48 μM, and impairs tumor cell migration concomitant with loss of microfilaments. [1] ABC294640 induces nonapoptotic cell death, morphological changes in lysosomes, formation of autophagosomes, and increases in acidic vesicles in A-498, PC-3, and MDA-MB-231 cells. [2] In both MCF-7 and ER-transfected HEK293 cells, ABC294640 decreases E2-stimulated ERE-luciferase activity. [3] |
| 体内活性 | In mice bearing mammary adenocarcinoma xenografts, ABC294640 (100 mg/kg, p.o.) significantly reduce tumor growth, associated with depletion of S1P levels. [1] In severe combined immunodeficient mice bearing A-498 xenografts, ABC294640 delays tumor growth and elevates autophagy markers. [2] ABC294640 protects against liver transplantation-induced inflammation and cross-talk between innate and adaptive immunities, major events precipitating and exacerbating graft injury, and improves liver function and survival. [4] |
| 存储条件 | Store at low temperature,Store under nitrogen,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 27 mg/mL (70.88 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.25 mM), Sonication is recommended. DMSO : 71 mg/mL (186.4 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | SphK2 | SphK | Sphingosine kinase | S1PReceptor | S1P Receptor | Opaganib | Inhibitor | inhibit | ABC-294640 | ABC 294640 |
| 相关产品 | Sphingosine-1-phosphate | Siponimod | W140 HBr | BMS-960 | Ozanimod | LX-2931 | Etrasimod | SLP9101555 | MP-A08 | CYM50374 | Fingolimod hydrochloride | ASP-4058 |
| 相关库 | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | Kinase Inhibitor Library | Anti-Viral Compound Library | GPCR Compound Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound 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 ABC294640【915385-81-8】
￥206 - 4120
