c-Met (HGFR) Kinase Targeted Library

c-Met, also known as MET or hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase that is frequently deregulated in human cancers. c-Met signaling pathway has a key role in invasive growth during embryonic development and postnatal organ regeneration. c-Met can induce several biological process in response to HGF stimulation, which together lead to a program known as invasive growth. c-Met signaling pathway is only fully activated during wound healing and tissue regeneration in adults, but the tumor c-Met signaling pathway can be frequently activated by cancer cells, contributing to tumor formation, invasive growth and metastasis. Currently, a variety of c-Met inhibitors with multiple chemical structures are under clinical investigation.

BOC Sciences has developed a c-Met (HGFR) protein kinase targeted library containing diverse potentially selective c-Met inhibitors.

Figure 1. Schematic diagram of the cAMP/PKA signalling pathway. (Han, P.; et al. 2017)

Library Design

BOC Sciences’ screening compound library of selective c-Met inhibitors is designed based on comparing key amino acids in the protein binding site with the characters of known potent inhibitor.

1. Firstly, we apply the X-ray structure of the protein recorded in the PDB entry to establish the docking model of c-Met kinase binding site
2. Then, a reference subset of known inhibitors from the database is used to validate the screening model
3. The key amino acids involved in ligand binding are identified by molecular docking of known active compounds
4. In this step, we prepare a well-designed query model of the protein binding site using the screening tool. The query model includes the following features: acceptor and donor sites, hydrophobic regions and surface volume constraints of the protein
5. Finally, the entire BOC Sciences compound collections are processed using our in-house filters to detect and remove PAINS compounds. Moreover, the filtering procedure is applied subsequently to a set of pre-filtered BOC Sciences HTS compounds by employing various flexible search options and feature constraint limits

c-Met (HGFR) Kinase Targeted 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

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 c-Met (HGFR) Kinase Targeted Library design at competitive prices for global customers. Personalized and customized services of c-Met (HGFR) Kinase Targeted 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!