csf-1r

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Sotuletinib (BLZ945) is a CSF-1R inhibitor, a highly selective, brain-penetrant CSF-1R inhibitor (IC50 = 1 nM, with 1000-fold selectivity over other kinases), with oral activity, used for microglia depletion and tumor and neurological disease research.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation. This product is also available as a premixed diet version (C2005 PLX5622 in AIN-76A Diet (1200 ppm)), eliminating the need for self-preparation and offering superior stability and reproducibility.

c-Fms-IN-8 is a colony-stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor (IC50: 9.1 nM). It is compound 4a in the reference.

Vimseltinib (DCC-3014) is a dual inhibitor targeting c-FMS (CSF-IR) and c-Kit with IC50 values of less than 0.01 μM and 0.1-1 μM, respectively.

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) inhibitor.

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

ARRY-382 is a highly selective oral inhibitor of CSF-1R with an IC50 of 9 nM.

Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC50 value of 2.1 nM. CSF1R-IN-3 has anti-proliferative activity against colorectal cancer cells. CSF1R-IN-3 exhibits anti-tumour effects and immune enhancing effects by inhibiting the migration of macrophages and inducing the reprogramming of M2-type macrophages to M1-type macrophages, thus exhibited activity against colorectal cancer cells.

Mavrilimumab (CAM 3001) is a monoclonal antibody with antiviral activity that targets the α subunit of the granulocytic-macrophage colony-stimulating factor (GM-CSF) receptor, inhibiting downstream intracellular GM-CSF signaling. GM-CSF may contribute to an overactive inflammatory response linked to respiratory failure and death and could be used to study rheumatoid arthritis.

Axatilimab (SNDX-6352) is a human IgG4 antibody targeting the colony-stimulating factor 1 receptor (CSF-1R), which can be used for the study of immune system disorders and respiratory diseases.

Otilimab (GSK 3196165) is a humanized monoclonal antibody against granulocyt-macrophage colony-stimulating factor (GM-CSF). Otilimab has anti-inflammatory activity, regulates the biological function of GM-CSF by blocking the interaction between GM-CSF and its cell surface receptors, and can be used in studies to treat severe COVID-19 pneumonia.

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).

CSF1R-IN-1 is a CSF1R inhibitor with an IC50 of 0.5 nM.

CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).

PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).

GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS.

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.