rapifleX®MALDI PHARMAPULSE®
High-Throughput Screening
Unique speed and specificity offered by label-free MALDI-TOF mass spectrometry
Highlights
rapifleX®MALDI PHARMAPULSE®
Eigenschaften
rapifleX®MALDI PHARMAPULSE®
全新的Rapiflex®MALDI飞行时间质谱仪是MaldiPharmapulse®的核心，它结合了Brukers最新的10 kHz扫描激光技术，每秒可以读取多个样品。系统的所有组件共同用于全自动HTS操作。新设计的筛选软件套件支持HTS工作流程，并与专有测定开发模块合并，该模块使测定者能够加速MALDI质谱法的无标签测定开发。Rapiflex®MPP的最新综合筛选'软件模块为例如在高速度下监测化学反应或在无与伦比的高吞吐量和特异性下对结合测定的分析。
rapifleX®MALDI PHARMAPULSE®（MPP）通过大型物质的大型化合物库梳
质谱法的使用允许测量主要屏幕中未修饰的底物，以避免误报或假阴性，从而使确认屏幕冗余。该系统设计用于全自动处理384和1536个样品板，以筛选一周的一周以上化合物以支持药物发现。
New standard for ultra-High-Throughput Screening Label-Free ‘Hit’ Identification
By combining the speed of Bruker’s patented smartbeam 3D laser technology with the direct-detection capability of mass spectrometry, the rapifleX®MPP提供了前所未有的筛查能力，用于对生化和细胞测定的超高通量筛查。它使您可以以每周超过一百万个化合物的速度筛选大型和多样化的化合物库，从而代表了自动化和微型化的完美平衡。
We are very proud to be the first CRO having integrated Bruker’s rapifleX mass spectrometer as read-out technology into our uHTS system. Mass spectrometry allows the direct measurement of label-free assays and reduces the number of false positives and false negatives in our screen, which makes the hit to lead phase of our drug discovery program more time and cost effective.
Robustness to analyze 2-3 million samples without intervention
- New source and ion optical design
- 即使在主屏幕中也没有源/离子光学清洁
- 如果需要的话，便于快速清洁
Compatible with CyBio®- 与384或1536通道的同时移液器保持较高精度和超快速样品板制备。
Single digit cost per sample
- No LC solvents, no waste, no labeling
- 0.025 to 1 μL sample volume
- Low cost disposable sample plates
全自动1536样板变化
- New ultra-fast autoloader seamlessly integrable with common robot systems
- Rugged design tailored for uHTS operation
New disposable MALDI HTS sample plates
- Fulfills all requirements for reliable MALDI ionization
- Suitable for 384, 1536, 3072 or 6144 geometries
Vorteile
Rafiflex®MPP有助于测定开发，加速HTS和UHTS命中发现，并支持HIT确认和铅优化
The MPP system allows for the measurement of unmodified substrates in primary biochemical screens, and offers several advantages:
- It effectively eliminates confirmatory assays typically required of traditional fluorescence-based screening techniques
- 节省开发特定荧光探针或抗体的成本
- Doesn’t require expensive solvents or consumables for continuous operation
- 允许样品体积降至25 nl
PharmaPulse Solution
The PharmaPulse Solution is based on Bruker´s advanced MALDI-TOF technology and on a dedicated software package. Ease of use and time to result were key drivers during the development resulting in an intuitive but yet powerful software solution to measure and analyze millions of samples in full automation. Two workflows guide the user from adapting an assay to MALDI mass spectrometry to readily exported results for further analysis in LIMS systems.
New software module supports synthesis screening and binding assays
In biochemical screening experiments, the rapifleX®MPP决定了生物化学的转化率ical assay when performed in the presence of potential inhibitors. In such a screen, a distinct MS peak ratio comparing product and substrate intensities is monitored throughout large numbers of sample spots, where each spot represents the same biochemical conversion reaction, but measures the effectiveness of a different inhibitor molecule.
In addition to this screening functionality, the new MPP software module supports “Synthesis Screening”, a methodology that requires more flexibility with regard to m/z values to be targeted by MALDI-TOF MS. Here, m/z values of interest may vary from spot to spot as each sample may represent a different chemical reaction. Accordingly, the new MPP “Synthesis Screening” software module allows scientists to screen for a large number of compounds per individual sample spot. This new MALDI-TOF based high-throughput analysis workflow could, therefore, enable highly time-efficient surveying of chemical reactivity landscapes at previously unseen mapping depth.
安温登根
rapifleX®MPP – the universal tool for drug discovery
完整的库屏幕
Rafiflex®MPP is the only mass spectrometer for large primary screens of millions of compounds with high diversity. Full automation supports screening of more than one million compounds per week, avoiding time-consuming confirmatory screens. [1]
集中的库屏幕
The quality of data obtained with rapifleX®MPP meets the requirements of secondary and confirmatory screens and makes it the ideal detector for focused library screens, such as the identification of kinase inhibitors of a target protein from a smaller subset of the library. [2]
片段筛选
The mass range and resolution accessible by MALDI-TOF mass spectrometry enables screening of fragments and other low molecular weight compounds. [3]
[1] Winter, M.; Ries, R.; Kleiner, C.; Bischoff, D.; Luippold, A. H.; Bretschneider, T.; Buettner, F. H.; Automated MALDI Target Preparation Concept: Providing Ultra-High-Throughput Mass Spectrometry–Based Screening for Drug Discovery. SLAS Technology 2018, https://doi.org/10.1177/2472630318791981
[2] Beeman，K。;Baumgartner，J。；Laubenheimer，M。；K. Hergesell；霍夫曼（M。）pehl，u。Fischer，F。;Pieck，J.C。;基于原位MALDI的高通量筛查过程的整合：与受体酪氨酸激酶C-MET的案例研究。SLAS光盘。 2017, 22, 1203–1210.
[3] VanderPorten, E.; Scholle, M.; Sherrill, J.; et al. Identification of Small-Molecule Noncovalent Binders Utilizing SAMDI Technology. SLAS Discov. 2017, 22(10):1211-1217.
目标评估和命中确认
对酶生物化学和动力学的透彻了解对于开发和验证强大的HTS分析至关重要。Rapiflex®MPP assists assay development and hit confirmation with linearity tests, substrate selection, Ki measurements and IC50 determination.
IC50 determination of inhibitors
半最大抑制剂浓度（IC50）是药物发现过程中的关键参数。MALDI PHARMAPULSE®software supports assay development by featuring a dedicated method development module. Optimal assay conditions obtained using the method development module are applied during MALDI-TOF screening, for example aiming for IC50 determination, which is set up and executed in the software´s dedicated screening module.
rapifleX®MPP – for primary screening
每周使用Rapiflex一百万样品®MALDI PHARMAPULSE®
新的Rafiflex®MPP是Bruker创新的MALDI质谱仪的结果。它反映了我们对这项技术及其独特应用的热情和知识。Rapiflex的飞行时间质谱仪（TOF MS）®MALDI PHARMAPULSE®在HTS模式下监测高达30块质量：从小分子到大蛋白。Rapiflex的分辨率和灵敏度的提高®TOF MS allows e.g. the monitoring of acetylcholine (ACh) and choline to identify acetylcholinesterase (AChE) inhibitors out of millions of substances. An ingenious detector design delivers significantly improved signal to noise ratios for enhanced sensitivity across the mass range. A completely new HTS software suite supports easy set-up of HTS screens, and the proprietary assay development module ensures fast adaption of label-free assays for MALDI mass spectrometry.
Automation of rapifleX®MALDI PHARMAPULSE®
Rafiflex®MALDI PHARMAPULSE®is designed to seamlessly integrate with laboratory automation systems to perform fully automatic screening campaigns. The MALDI PharmaPulse®软件解决方案提供了一个开放的接口，可以从外部调度软件（例如Analytik Jena Lab Automation，Hightr Res Biosolutions，Beckman Coulter，Thermo Scientific Automation）控制其操作的一部分。Rapiflex的新高速自动装箱®MPP与机器人系统并驾齐驱，可快速加载和卸载样品板。
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For Research Use Only. Not for use in clinical diagnostic procedures.