rapifleX®MALDI PharmaPulse®
High-Throughput Screening
无标签的MALDI-TOF质谱法提供的独特速度和特异性
Punti salienti
rapifleX®MALDI PharmaPulse®
Caratteristiche
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.
New standard for ultra-High-Throughput Screening Label-Free ‘Hit’ Identification
通过将Bruker专利的SmartBeam 3D激光技术的速度与质谱的直接检测能力相结合，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.
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.
坚固to analyze 2-3 million samples without intervention
- 新来源和离子光学设计
- No source/ion optic cleaning even within primary screens
- Easy and fast cleaning if required
Compatible with CyBio®-Well vario with 384 or 1536 channel simultaneous pipettor for high precision and ultra-fast sample plate preparation.
每个样本的单位数字
- 没有LC溶剂，没有浪费，没有标签
- 0.025 to 1 μL sample volume
- 低成本的一次性样品板
全自动1536样板变化
- New ultra-fast autoloader seamlessly integrable with common robot systems
- 为UHTS操作量身定制的坚固设计
新的一次性Maldi HTS样品板
- Fulfills all requirements for reliable MALDI ionization
- Suitable for 384, 1536, 3072 or 6144 geometries
Benefici
The rapifleX®MPP assists assay development, accelerates HTS and uHTS hit finding, and supports hit confirmation and lead optimization
MPP系统允许在原发性生化筛选中测量未修饰的底物，并提供多个优点：
- It effectively eliminates confirmatory assays typically required of traditional fluorescence-based screening techniques
- Saves costs for developing specific fluorescence probes or antibodies
- Doesn’t require expensive solvents or consumables for continuous operation
- Allows sample volume down to 25 nL
PharmaPulse Solution
Pharmapulse解决方案基于Bruker的高级MALDI-TOF技术和专用软件包。在开发过程中，易于使用和时间是关键驱动因素，从而产生了直观但功能强大的软件解决方案，以测量和分析数百万个完全自动化的样本。两个工作流程指导用户从对MALDI质谱进行调整，以便在LIMS系统中进一步分析结果。
New software module supports synthesis screening and binding assays
In biochemical screening experiments, the rapifleX®MPP确定在存在潜在抑制剂的情况下进行生化测定时的转化率。在这样的屏幕中，比较产物和底物强度的明显MS峰值比在大量样品斑中进行监测，其中每个斑点代表相同的生化转化反应，但测量了不同抑制剂分子的有效性。
除了此筛选功能外，新的MPP软件模块还支持“综合筛选”，该方法学需要更高的灵活性，以实现MALDI-TOF MS的目标。在这里，感兴趣的M/Z值可能因点而异，因为每个样品可能代表不同的化学反应。因此，新的MPP“合成筛选”软件模块允许科学家筛选每个样品点的大量化合物。因此，这项新的基于MALDI-TOF的高通量分析工作流可以使高度及时的化学反应性景观的测量深度在以前看不见的映射深度上进行测量。
应用
rapifleX®MPP – the universal tool for drug discovery
Full library screens
The rapifleX®MPP是数百万种具有高度多样性化合物的大主筛网的唯一质谱仪。完全自动化支持每周超过一百万种化合物的筛查，避免了耗时的确认屏幕。[1]
Focused library screens
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]
Fragment screening
通过MALDI-TOF质谱法可以访问质量范围和分辨率，可以筛选片段和其他低分子量化合物。[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.; 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大肠;Scholle m;谢里尔,j .;et al. Identification of Small-Molecule Noncovalent Binders Utilizing SAMDI Technology. 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 assists assay development and hit confirmation with linearity tests, substrate selection, Ki measurements and IC50 determination.
IC50 determination of inhibitors
Half-maximal inhibitor concentration (IC50) is a key parameter in the drug discovery process. 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 - 主要筛查
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 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.
Rapiflex的自动化®MALDI PharmaPulse®
The rapifleX®MALDI PharmaPulse®is designed to seamlessly integrate with laboratory automation systems to perform fully automatic screening campaigns. The 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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For Research Use Only. Not for use in clinical diagnostic procedures.