mast/stem

M4205 is an inhibitor of c-Kit exhibiting high activity on c-Kit mutations in exons 11, 13, 17.

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT).

Briquilimab (JSP-191) is a humanized, aglycosylated monoclonal antibody that directly inhibits the interaction between the stem cell factor (SCF) ligand and its receptor, KIT (CD117), leading to the blockade of the downstream KIT signaling pathway and ultimately inducing mast cell apoptosis; the SCF-KIT interaction is well-characterized as essential for mast cell survival, and its inhibition has been demonstrated to directly trigger mast cell apoptosis primarily through the Bim-mediated pathway, thereby removing the underlying cellular source of inflammation for many immunological and inflammatory diseases, including chronic urticaria and asthma.