rapifleX®MALDI PharmaPulse®
高通量筛选
Unique speed and specificity offered by label-free MALDI-TOF mass spectrometry
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rapifleX®MALDI PharmaPulse®
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rapifleX®MALDI PharmaPulse®
The all new rapifleX® MALDI Time-of-Flight mass spectrometer is the heart of the MALDI PharmaPulse®, it incorporates Brukers latest 10 kHz scanning laser technology and can read multiple samples per second. All components of the system work in concert for fully automatic HTS operation. The newly designed screening software suite supports HTS workflows and works in combination with a proprietary assay development module which empowers assay developer to accelerate label-free assay development for MALDI mass spectrometry. The latest ‚Synthesis Screening‘ software module of the rapifleX® MPP opens a new application space for e.g. monitoring of chemical reactions at high pace or analysis of binding assays at incomparable high throughput and specificity.
rapifleX®MALDI PharmaPulse®(MPP) combs through large compound libraries of millions of substances
The use of mass spectrometry allows the measurement of unmodified substrates in primary screens to avoid false positives or false negatives, making confirmation screens redundant. The system is designed for fully automatic handling of 384 and 1536 sample plates to screen more than a million compounds in a week in support of drug discovery.
超高通量筛查标签的“命中”标识的新标准
By combining the speed of Bruker’s patented smartbeam 3D laser technology with the direct-detection capability of mass spectrometry, the rapifleX®MPP delivers unprecedented screening capability for ultra high-throughput screening of biochemical and cellular assays. It allows you to screen through large and diverse compound libraries at a pace of over a million compounds a week, epitomizing the perfect balance of automation and miniaturization.
我们很荣幸能成为第一个将Bruker集成的Rapiflex质谱仪作为读出技术进入我们的UHTS系统的CRO。质谱允许直接测量无标签测定法，并减少屏幕上的假阳性和假阴性的数量，从而使我们的药物发现计划的领先阶段更加时间和成本效益。
鲁棒性分析2-300万样品而无需干预
- New source and ion optical design
- No source/ion optic cleaning even within primary screens
- Easy and fast cleaning if required
与Cybio兼容®-Well vario with 384 or 1536 channel simultaneous pipettor for high precision and ultra-fast sample plate preparation.
Single digit cost per sample
- No LC solvents, no waste, no labeling
- 0.025至1μl样品体积
- Low cost disposable sample plates
全自动1536样品板更改
- 新的超快速自动加载器与普通机器人系统无缝集成
- Rugged design tailored for uHTS operation
New disposable MALDI HTS sample plates
- 满足可靠的Maldi离子化的所有要求
- 适用于384、1536、3072或6144几何形状
혜택
The rapifleX®MPP assists assay development, accelerates HTS and uHTS hit finding, and supports hit confirmation and lead optimization
The MPP system allows for the measurement of unmodified substrates in primary biochemical screens, and offers several advantages:
- 它有效地消除了通常需要基于传统荧光的筛选技术所需的验证性测定
- Saves costs for developing specific fluorescence probes or antibodies
- 不需要昂贵的溶剂或消耗品即可连续操作
- Allows sample volume down to 25 nL
Pharmapulse溶液
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.
新软件模块支持合成筛选和绑定测定
在生化筛选实验中，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.
응용
rapifleX®MPP - 药物发现的通用工具
Full library screens
The rapifleX®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]
Focused library screens
用Rapiflex获得的数据质量®MPP满足了继发性和验证性筛选的要求，使其成为集中库筛选的理想检测器，例如从较小的库中识别靶蛋白的激酶抑制剂。[2]
Fragment screening
The mass range and resolution accessible by MALDI-TOF mass spectrometry enables screening of fragments and other low molecular weight compounds. [3]
[1]冬季，M。；Ries，R。;克莱纳（C.）Bischoff，d。;Luippold，A。H。;Bretschneider，T。Buettner，F。H。;自动化的MALDI目标制备概念：提供基于药物发现的超高通量质谱法筛查。SLAS Technology 2018，https://doi.org/10.1177/2472630318791981
[2]Beeman, K.; Baumgartner, J.; Laubenheimer, M.; Hergesell, K.; Hoffmann, M.; Pehl, U.; Fischer, F.; Pieck, J.C.; Integration of an In Situ MALDI-Based High-Throughput Screening Process: A Case Study with Receptor Tyrosine Kinase c-MET. SLAS Disc. 2017, 22, 1203–1210.
[3] Vanderporten，E。；Scholle，M。；Sherrill，J。；等。利用SAMDI技术的小分子非分子粘合剂的鉴定。Slas Discov。2017，22（10）：1211-1217。
Target evaluation and hit confirmation
Thorough understanding of enzyme biochemistry and kinetics is essential to develop and validate robust HTS assays. rapiflex®MPP通过线性测试，底物选择，KI测量和IC50测定有助于测定开发并进行确认。
IC50测定抑制剂
Half-maximal抑制剂浓度(IC50)是一个key parameter in the drug discovery process. MALDI PharmaPulse®软件通过具有专用方法开发模块来支持测定开发。使用方法开发模块获得的最佳测定条件是在MALDI-TOF筛选期间应用的，例如，针对IC50确定，该确定是在软件的专用筛选模块中设置和执行的。
rapifleX®MPP – for primary screening
A million samples per week with rapifleX®MALDI PharmaPulse®
The new rapifleX®MPP is the result of Bruker’s innovative development of MALDI mass spectrometers. It reflects our passion for and knowledge about this technology and its unique applications. The time-of-flight mass spectrometer (TOF MS) of the rapifleX®MALDI PharmaPulse®monitors up to 30 masses in HTS mode: from small molecules to large proteins. The improved resolution and sensitivity of the rapifleX®TOF MS允许，例如对乙酰胆碱（ACH）和胆碱的监测以鉴定乙酰胆碱酯酶（ACHE）抑制剂中数百万物质。巧妙的探测器设计可显着提高信号与噪声比，以提高整个质量范围的灵敏度。全新的HTS软件套件可轻松设置HTS屏幕，专有测定开发模块可确保快速适应MALDI质谱的无标签测定法。
Automation of rapifleX®MALDI PharmaPulse®
The rapifleX®MALDI PharmaPulse®旨在与实验室自动化系统无缝集成以执行全自动筛选活动。Maldi Pharmapulse®software solution offers an open interface to control parts of its operation from external scheduling software (e.g. Analytik Jena lab automation, HighRes Biosolutions, Beckman Coulter, Thermo Scientific automation). The new high-speed autoloader of the rapifleX®MPP works hand in hand with robot systems for quick loading and unloading of sample plates.
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