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CaliperLabChip3000 ® HTS Drug Discovery System

The LabChip 3000 system is Caliper's next generation
microfluidic system for use i drug screening. Using cutting
edge microfluidic technology, the LabChip 3000 Drug
Discovery System enables you to perform a broad range of
assays on a single integrated platform. The precision of microfluidics
allows researchers to detect subtle interactions between
drug candidates and therapeutic targets. The technology
is able to detect both strong and weak inhibitors with high
accuracy, and routinely identifies drug candidates that conventional
techniques miss. The flexibility of the LabChip 3000 System allows its use throughout the drug discovery process including assay development, primary screening, selectivity screening and generation of structure-activity relations (SARs). Most important therapeutic enzymatic 'targets' such as kinases, proteases and phosphatases can be screened using the LabChip 3000 System. The system also performs miniaturized cell based GPCR screens.

Dverse Assay Menu

A variety of enzymatic and cell-based assays can be performed on a single CaliperLS HTS3000instrument. The assay menu for the CaliperLS HTS3000includes:

• Serine/Threonine Kinases;
• Tyrosine Kinases;
• Phosphatases;
• Proteases;
• Lipid-modifying Enzymes; and
• G-protein coupled receptors (GPCRs).

Caliper's most recent introduction, KiSS (Kinase Selectivity Screening) offers lead optimization and secondary screening laboratories
a simple, affordable approach to kinase profiling.

Software screen dumps

Two Configurations to Meet your Laboratory's Needs

Depending on the system configuration you select, the CaliperLS HTS3000is well suited to all areas of drug discovery:

• Assay Development
• Primary Screening
• Secondary/Selectivity Screening
• Lead Optimization

Simple, low-cost Assay Development Stations allow for method development and low-throughput screening requirements. Screening systems
meet the needs of medium- and high-throughput screening laboratories, and come equipped with an on-board Twister™ plate handler. An
environmental control chamber is also included with the screening system so that 96- and 384-well plates can be automatically processed
without risking sample evaporation.

Sipper Chips for Higher Throughput

The CaliperLS HTS3000uses Caliper's proprietary sipper chips as the "chip-to-world" interface that allows automated sampling from microtiter plates.
To meet the needs of higher-throughput environments, the CaliperLS HTS3000employs four or even twelve sippers on a single chip - so that
samples can be processed, in parallel, up to twelve at a time.

Once on the chip, samples are manipulated through the channels of the chip to perform the steps required for mixing, incubation,
reaction, separation, and detection. Movement through the channels is controlled using a combination of pressure and/or voltage, as
described in the Technologies section.

Separations-based Assays for Analytical Quality Data

With Caliper's mobility shift enzymatic assays, the product and substrate are electrophoretically separated, thereby minimizing
interferences and yielding the highest data quality available on any screening platform. Z' factors for CaliperLS HTS3000enzymatic assays
are routinely in the 0.8 to 0.9 range.

For cell-based assays, cells move past the detector one at a time, so that they can be measured independently, and so that potentially
interfering fluorescent compounds do not interfere. The result is fewer false positives and more confidence in your screening data.

Microfluidic Format Saves Precious Reagents

The channels of the LabChip devices are 10-50um in diameter, which means that many LabChip assays use much less reagent than
would be required for the equivalent plate-based assay. For example, customers running cell-based calcium flux assays on a
CaliperLS HTS3000report using 100 times fewer cells per datapoint compared to their equivalent plate-based assays. For scientists constrained
by limited cell availability, e.g. those working with primary cell lines, this offers a way to perform more assays than would otherwise be possible.

Real Successes in Big Pharma

Millennium, Amgen, Lilly, Wyeth, Amgen, and other pharmaceutical companies are actively using Caliper systems as key tools in their screening
efforts. The most cited reason for using the Caliper system? Data quality. High Z' values, few false positives, few false negatives and
analytical quality reproducibility are the reasons cited for the increasing reliance on the CaliperLS HTS3000.

Read more about microfluidics role in the drug discovery effort in the following publications:

Studt, T. Building Lab-on-a-Chip Technology Platforms. Drug Discovery and Development 2002, 5 (6), 32-37.
view article online
Millennium Pharmaceuticals' Vice President of Platform Technologies is interviewed about how LabChip technology has been successfully
integrated into his HTS programs.

Johnson, M., et al. Converting a Protease Assay to a Caliper Format LabChip System. JALA 2002, 7(4), 62-68.
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Amgen publishes the results of their efforts to transfer a protease assay from plate-based to LabChip format.

Pearson, Sue. Identifying Novel Targets in the Post-Genomic Era. Genetic Enginerering News 2002, 22(20), 62-63.
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Overview of novel screening approaches, including Amphora Discovery Corp.'s "chemical genomics" approach that relies on
"intervention-free detection" using Caliper's drug discovery platform.

"Twister" is a trademark of Zymark Corporation