C-MET KINASE INHIBITORS

c-Met (MET or mesenchymal-epithelial transition factor) is a prototype member of a subfamily of heterodimeric receptor tyrosine kinases (RTKs) and is the receptor for a hepatocyte growth factor (HGF). MET can be activated through ligand-dependent or independent mechanisms. The binding of HGF to the extracellular MET domain results in receptor multimerization, phosphorylation, and activation of MET-dependent signal transduction within the cell.

Activation of the MET receptor leads to subsequent signal activation, including mitogen-activated protein kinase (ERK / MAPK) and phosphatidylinositol 3-kinase (PI3K / AKT), STAT3, and RAS pathways. Dysregulated HGF / c-Met signaling is a driver of several malignancies and promotes tumor growth, invasion, spread, and angiogenesis. Dysregulated HGF / c-Met signaling has also been associated with poor clinical outcomes and acquisition of resistance to some approved targeted therapies. Thus, c-Met kinase has become a promising target for anticancer drug development.

Different therapeutic approaches targeting the HGF / c-Met signaling pathway are being developed for targeted therapy against cancer, among which small molecule c-Met kinase inhibitors constitute the largest effort within the pharmaceutical industry. BioVision is proud to offer several structurally diverse small molecule c-Met kinase inhibitors for research.

With nearly two decades of experience in drug kinase discovery, Eurofins Discovery has developed the largest collection of nearly 500 biochemical and cellular kinase assays that enable rapid determination of the potency and selectivity of compounds throughout the kinome. Screening your compounds against the largest panel of single wild-type human kinases available allows you to make better-informed decisions about therapeutic opportunities and potential off-target responsibilities that might otherwise be missed in smaller kinase panels.

For couples with the fastest turnaround time in the industry, Eurofins Discovery’s kinase detection and profiling services enable accelerated SAR testing to advance those compounds that have the biggest change from being clinically effective and safe, as fast as possible.

We offer various cell-based and biochemical kinase assay platforms that enable the development of complete drug kinase discovery programs from an HTS screen to Hit to Lead (HTL) and prospect optimization. We can build a complete screening cascade for an HTL program that allows the selection of a leading candidate.

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