Information-rich kinetic binding data lets you understand measures critical to determining clinical efficacy. Agile R100 is a novel label-free orthogonal assay for small molecule and protein hit validation that can detect interactions in complex solutions with just a 10 µL drop of sample. Characterize your candidates earlier in the process – and reduce costly mistakes further down the line.
Easily gain sensitive label-free data including:
- Kinetic binding data and analysis
- Affinity ranking
- Dissociation rates
- Concentration measurements
AGILE R100 FEATURES
- Complex sample use enables detection in up to 10% DMSO, cell or tissue lysate, and cell growth supernatant.
- Microfluidics-free design means no clogging or maintenance that requires annoying service contracts.
- Single-sample format lets you modify your assay mid-experiment.
- Reusable biosensor chip provides up to 10 measurements.
- Easy-to-learn instrument requires minimal training.
- Agile Plus software makes running assays and data analysis easy.
Kinetic binding data at the early stages of drug discovery can provide advance insight into the biological activity profile of your compounds. Easily run assays at your bench in a free afternoon to characterize lead compounds and make confident decisions regarding your candidates.
Choose one of the below applications to learn more:
Built with breakthrough Field Effect Biosensing (FEB) technology, Agile R100 biosensor chips help you fully characterize and explore your interactions to make better decisions earlier. The surface of the biosensor chip is made of graphene, platinum, and glass – biologically inert materials that do not react with your experiment and cause unnecessary nonspecific binding.
Each biosensor chip is built with graphene transistors which provide a minimum of 3 replicate data points per measurement for strong internal reproducibility and technical control. Depending on the stability of the immobilized molecule, each chip can provide 10 measurements.
The Agile R100 reader (not shown) houses the majority of the system’s electronic components. The Agile R100 cartridge holds the biosensor chip and biological materials. It is easy to clean, and an included clear cover reduces liquid evaporation.
The cartridge can connect directly to the reader for compact use and can be separated from the reader post-experiment for easy decontamination with standard protocols.
The cartridge can also attach to the reader via a one-meter-long high density cable, which is an optional accessory. This enables additional use of the cartridge in a wide range of experimental settings (ex: with a temperature controlled incubator or in a biosafety cabinet) that may otherwise damage the reader.
The Agile R100 reader houses the majority of the platform’s electronic components and powers the system via a USB connection to a computer or laptop. The reader can connect directly to the cartridge for compact use or be separated via a one-meter-long high density cable, which is an optional accessory. This enables a wide range of experimental settings (ex: with a temperature controlled incubator or in a biosafety cabinet) by providing the ability to use the cartridge in conditions that may otherwise damage the reader.
We are committed to helping you capture the best data possible with your Agile R100 platform. Highly-trained and qualified Field Applications Scientists partner with you at your lab or facility to train any size party on how to use Agile R100 to generate high-quality kinetic binding and affinity data at your bench.
The agenda is customizable to your needs, and topics can include the basics of Field Effect Biosensing (FEB) technology, assay development with Agile R100, data acquisition and analysis software use, analysis interpretation, maintenance, cleaning, and troubleshooting.
WORKFLOW AND SENSORGRAM
|Dynamic Range of Detection||100 fM - 10 mM|
|Sample Volume||10-50 uL|
|Functionalization Amount||0.5-500 ng of material|
|Temperature Range||-20C to 100 C|
|Lower Sense of Time||2 minutes|
|Upper Sense of Time||8+ hours|
|Size of Immobilized Target||1 Da-200 kDa|
|Size of Analyte in Solution||1 Da-200 kDa|
|Sample Type||Small molecules in ≤ 10% DMSO, cell & tissue lysate, blood fractions|
|Target Chemistry||EDC/sNHS or His-tag linkage|
|Speed of Data Collection||Up to 420 points/min|
|Shelf Stable||3-6 months, stored with desiccant|
|Number of Measurements||Up to 10 per Agile biosensor chip|
|Computer Specifications||PC with USB port, Windows 7 or later|
|Product Dimensions||9 in. x 3 in.|
Agile R100 versus MicroCal iTC200 Kinetic Binding DataLogin
Agile R100 is a graphene biosensor with unprecedented functionality, providing label-free, real-time kinetic binding data. As a novel technology, Agile R100 is compared to MicroCal iTC200 to demonstrate its benefits compared to a standard kinetic binding analysis tool, isothermal titration calorimetry (ITC). In this study, kinetic binding data between the two instruments is compared by measuring Rho guanosine triphosphate hydrolase enzyme (GTPase) interacting with GTPase activating protein (GAP). The association and dissociation binding rate (ka and kd, respectively) and dissociation constants (KD) are reported. Agile R100 has a precise binding affinity measurement (KD = 1.35 ± 0.06 µM), comparable to MicroCal iTC200 (KD = 2.7 ± 0.3 µM), while also obtaining ka and kd values. Additionally, Agile R100 uses up to 30 million times less sample material and up to 30 times less sample volume and can perform 2.5 times more measurements in a given workday compared to MicroCal iTC200.
Detecting Interactions of Small Molecules in DMSO Using Agile R100Login
Small molecules are beneficial as drug therapeutics but often have low solubility in aqueous solutions. Solvents such as dimethyl sulfoxide (DMSO) are necessary additives for small molecule solubility, but these solvents can interfere with optical biosensing platforms. In this technical note, Agile R100 successfully detects the interaction between the cytokine tumor necrosis factor alpha (TNFα) and the small molecule inhibitor SPD304 in 0%, 1%, 3%, and 10% DMSO. Because Agile R100 uses an electrical technique rather than an optical one, DMSO in buffer is compatible with the instrument and does not require solvent correction. Additionally, high concentrations of SPD304 (100 μM) were detected on Agile R100. Importantly, Agile R100 detects the association binding rate (ka) and the dissociation binding rate (kd) and can calculate the dissociation constant (KD) of the TNFα and SPD304 interaction in buffer with DMSO. Agile R100’s KD result (14.5 ± 1.8 μM in phosphate buffer saline [PBS] with 10% DMSO) is similar to a previously reported KD value (7.3 ± 0.5 μM in citrate phosphate buffer with 10% DMSO).
Affinity Ranking of SPD304, Evans Blue, and Trypan Blue to TNFα Using Agile R100Login
Affinity ranking is critical to optimizing the relationship between a target protein and a potential drug compound during the hit-to-lead optimization phase of drug discovery. In this application note, Agile R100 characterizes the activity of the target protein TNFα interacting with the small molecule drug compounds, SPD304, Evans Blue, and Trypan Blue in order to rank order by affinity.