ASINEX - Chemical Solution Provider

ASINEX has been providing drug discovery services and chemical solutions since 1994. The HQ is in Moscow and we have offices in the USA, The Netherlands and Japan. ASINEX is most well known as a supplier of high value chemical libraries, having designed and synthesized 1,000 novel chemotypes during the last five years.

However, ASINEX is also a service provider, half of our 120 chemists (50 PhDs) work on a service basis for our clients. We have a large bioscreening department of 30 biologists (20 PhDs) who are able to provide custom screening and ADMET/PK services. Finally, we have an automated chemistry unit in the UK where we synthesize exclusive libraries and purification services.

ADMET AND PK STUDIES

ASINEX offers a wide range of ADMET services:

• Cytotoxicity: cell viability: human hepatocellular carcinoma cells / human and rat primary hepatocytes
• Drug transport assay (Caco-2 cell, 21 day culture)
• In vitro absorption: P-glycoprotein inhibition / PAMPA
• In vitro metabolism: CYP-450 / microsomes / S9 fraction / hepatocytes / half-life / plasma stability
• Herg Inhibition: [H3] astemizole binding to membranes of HERG transfected HEK293 cells
• Physiochemical properties: aqueous solubility / chemical stability / lipophilicty
• Proliferation and apoptosis: 18 cell lines
• We also offer PK studies

ASINEX recently initiated pharmacokinetics (PK) studies in vivo (rat or mice) in collaboration with a GLP accredited animal facility in Russia, in accordance with FDA (USA) and OECD (Europe) standards. ASINEX uses an LC-MS/MS technique to conduct the analytical part of the PK pre-clinical studies, using an Agilent 1200 Series LC platform, combined with an applied bio-systems 3200 QTrap MS/MS.

CUSTOM SCREENING / LEAD GENERATION

Our laboratories are equipped with modern HTS equipment and an unrivalled screening resource of 500,000 compounds. At ASINEX we routinely run cell-based and enzymatic assays for:

• Kinases
• GPCRs
• Proteases
• Phosphatases
• Transferases
• Enzymes
• Proteins from apoptosis signaling pathways

COMPOUND LIBRARIES

ASINEX’s expertise in library design derives from its experience as a service provider, and the development of our own advanced compound libraries requiring medicinal chemistry expertise and screening capabilities.

We have labeled our most recent in-house designed and synthesized libraries as ‘high-value’: libraries which deal with traditional problems such as false positives, re-supply, novelty, chemical stability, permeability and toxicity.

EXCLUSIVE LIBRARY SYNTHESIS

ASINEX can generate focused or high diversity libraries utilizing our comprehensive collection of 10,000 strategic building blocks. ASINEX has many years of experience in designing focused libraries against particular targets and in generating libraries which maximize or cover a particular area of chemical space. The ideal scenario is library generation based on ASINEX designed hit compounds.

LEAD OPTIMIZATION

ASINEX offers an integrated platform of biology and chemistry skills for hit to lead expansion and lead optimization. We are able to optimize hits from a multitude of sources and offer an especially fast service for ASINEX’s in-house designed compounds. Our scientists are able to optimize the following parameters: intellectual property, toxicity, solubility, permeability or metabolism.

CUSTOM SYNTHESIS

ASINEX’s main area of expertise is in hetero-cycle chemistry and multi-step synthesis of small molecule compounds including complex synthesis of poly-functional based compounds, protection / D-protection techniques, natural based analogues etc. ASINEX works from milligram to gram scale (up to 200g).

HIGH THROUGHPUT CHEMISTRY AND PURIFICATION

ASINEX has a fully integrated high-throughput chemistry, purification and analysis facility operating in the UK. We are capable of carrying out 8,000 chemical reactions and purifying up to 15,000 crude samples per month. All compounds synthesized undergo LC purification and LCMS data is provided for all samples shipped.

If high-throughput chemistry is feasible, a large number of compounds can be generated quickly and cost-effectively. ASINEX is able to generate a virtual library using the 20,000 reagents it has on the shelf. After initial test reactions have been carried out, a 50-80% success rate can be anticipated. High-throughput purification is also available on a service basis.