tumor-associated macrophages (tams)

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

CSF1R-IN-22 (Compound C19), a potent orally administered CSF-1R selective inhibitor (IC50 <6 nM), significantly enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration. Moreover, it amplifies the anti-tumor immune responses in conjunction with anti-PD-1 and triggers apoptosis in tumor cells. Additionally, CSF1R-IN-22 effectively reprograms M2-like TAMs (tumor-associated macrophages) to an M1 phenotype, modulates the tumor microenvironment (TME) by fostering the recruitment of CD8+ T cells, and diminishes the presence of immunosuppressive Tregs and MDSCs [1].

Emactuzumab(RG 7155) is a monoclonal antibody against colony-stimulating factor-1 receptor targeting tumor-associated macrophages (TAMs) Emactuzumab has antitumor activity and inhibits activation of colony-stimulating factor 1 receptor (CSF1R) Emactuzumab has a high affinity for CSF-1R with a Ki value of 0.2 nM. Emactuzumab blocks CSF-1R dimerization and can be used to study cancers such as diffuse tenosynovial giant cell tumor (dt-GCT).