MultiScreenHTS-PCF Filter plates for Solubility
Determining a compound's aqueous solubility has become an essential early measurement to make in the drug discovery process. Poor water solubility can cause problems in many different in vitro testing techniques leading to unreliable results and/or reproducibility problems; insoluble precipitates have been shown to cause false positives in bioassays potentially wasting valuable resources. Water solubility also influences absorption and thus can be used to help predict the bioavailability of a molecule.
Protocol
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| 1. | Add compound dissolved in organic solvent to aqueous buffer |
| 2. | Shake for 90 minutes to allow insoluble compound to precipitate |
| 3. | Apply vacuum to filter solution into collection plate. Precipitates remain on membrane. Analyze filtrate in collection plate to quantitate amount of compound still in solution |
Performance
Results Correlate to Shake-flask
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Fifteen (15) compounds were evaluated by an ASTM shake-flask method and a protocol using the MultiScreenHTS-PCF Filter plate. Shake-flask solubility was determined for solid compounds added to PBS. MultiScreenHTS-PCF Filter plate results were determined for 10 µL of 10 mM DMSO stocks added to 190 µL PBS for a final DMSO concentration of 5%. The maximum concentration on the Y axis is given as 500 µM due to the MultiScreenHTS-PCF Filter plate protocol that has an upper limit for the amount of compound added.
High Drug Recovery
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Soluble drugs were dissolved in 5% DMSO/PBS at 1 µM, incubated in the MultiScreenHTS-PCF Filter plate and filtered into a receiver plate. The results are reported as percent drug recovery as determined by radiometric analysis.
Validated for High Drug Recovery
The MultiScreenHTS-PCF Filter plate incorporates low-binding membrane and low-binding plate materials to yield the high drug recovery needed for solubility results. The plate is validated versus a panel of 9 drugs for >80% drug recovery at 10 µM concentration in 5% DMSO/PBS.
Increased Screening Throughput and Efficiency
The MultiScreenHTS-PCF Filter plate is a high
throughput, 96-well system to classify or quantify the aqueous solubility of
compound libraries stored in solvent as a concentrated solution.
The filtration-based protocol is fast and efficient. The protocol has been
validated to screen hundreds of samples per day and saves time and sample over
the shake-flask method. Typical MultiScreenHTS-PCF Filter plate
analysis time is less than 4 hours and uses <100 µg of sample per analysis.
This is an improvement as compared to the shake-flask method that can take
several days and require milligrams of sample for each analysis.
MultiScreenHTS-PCF Filter plates are automation compatible. The
plates are in compliance with SBS guidelines for easy handling by robotics.
They also include a space for barcoding.
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