ALK Tyrosine Kinase Focused Library

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor superfamily. ALK plays an important role in the development of the brain and exerts its effects on specific neurons in the nervous system: expressed mainly in specific regions of the central and peripheral nervous systems, and it plays an essential role in the genesis and differentiation of the nervous system. Currently, aberrantly expressed ALK tyrosine kinases have been found to be involved in the pathogenesis of various malignancies based on clinical data, and ALK genes have been rearranged, mutated or amplified in a wide range of tumors, including mesenchymal large cell lymphoma, neuroblastoma and non-small cell lung cancer. Given the close association of ALK with the development of multiple tumors, ALK inhibitors are identified for targeted therapy.

Aiming to provide drug-like screening compounds for over 2,500 potential anaplastic lymphoma kinase inhibitors, BOC Sciences has designed its proprietary ALK tyrosine kinase focused library.

Figure 1. Anaplastic lymphoma kinase (ALK) signaling in normal and cancer cells. (Takita, J. 2017)

Library Design

Step 1: We apply the data from a wide range of commercially available libraries of compounds to prepare a reference set of 8,000 biologically active compounds with reported activity against ALK including IC₅₀, Ki et al., ≤10 μM, inhibition >50%

Step 2: The BOC Sciences HTS compound collection is then used to searched for structural analogs of the compounds from the reference set by employing several 2D similarity methods and the 75% Tanimoto similarity cutoff

Step 3: Reactive, toxic and PAINS molecules will be carefully excluded from the screening library, and each compound is labeled with Rule of Five compliance

ALK Tyrosine Kinase Focused Library Characteristics

• Favorable physicochemical parameters and solubility requirements
• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Bioactivity and safety confirmed by preclinical studies and clinical trials
• Structural diversity, medicinal activity, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• All compounds are continually updated
• Compound cherry-picking service is provided

Figure 2. Anaplastic lymphoma kinase (ALK) expression in pediatric cancers detected by RNA sequencing. (Takita, J. 2017)

What We Deliver

• Delivered within 2 weeks in any customer-preferred format
• Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
• All compounds have a minimum purity of 90% assessed by ¹H NMR and HPLC
• Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of ALK Tyrosine Kinase Focused Library design at competitive prices for global customers. Personalized and customized services of ALK Tyrosine Kinase Focused Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!