c-FMS

Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.

CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.

CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

cFMS Receptor Inhibitor IV (Compound 42) is a potent cFMS inhibitor with an IC50 of 0.017 μM.

c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent.

Mavrilimumab (CAM 3001) is a monoclonal antibody that binds to the α subunit of the granulocyte-macrophage colony stimulating factor (GM-CSF) receptor and blocks intracellular signalling downstream of GM-CSF. GM-CSF might be a mediator of the hyperactive inflammatory response associated with respiratory failure and death.

Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab can enhance T cell infiltration and anti-tumor T cell immune response. Cabiralizumab inhibits osteoclast activation and prevents bone destruction, which can be used for research on rheumatoid arthritis (RA). Cabiralizumab can be combined with Nivolumab for lung cancer research.

JTE-952 is an orally active, type II selective inhibitor of colony-stimulating factor-1 receptor (CSF-1R/cFMS) that effectively inhibits CSF1R and TrkA with IC50 values of 13 nM and 261 nM, respectively. It can be used for research related to arthritis.

Sotuletinib (BLZ945) is an effective, selective, and brain-penetrant inhibitor of CSF-1R (c-Fms), with an IC50 of 1 nM and a selectivity that is 1000 times greater than other receptor tyrosine kinases.

Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R.

Otilimab (GSK 3196165) is an anti-granulocyte-macrophage colony-stimulating factor (GM-CSF) human monoclonal antibody.

GW2580-d6 is the deuterium labeled GW2580.

Pazopanib-13C,d3 (drochloride) is the deuterium and 13C labeled Pazopanib drochloride.

Pimicotinib is a CSF1R inhibitor with antitumor activity.

CSF1R-IN-24 (Example 134) is an orally active CSF1R inhibitor.

SYHA1813 is a dual inhibitor of CSF1R and VEGFR.

Anumigilimab (CSL-324) is an human IgG4 mAb against human granulocyte colony-stimulating factor (G-CSF) receptor.