colony stimulating factor 1 receptor

Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.

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

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.

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.

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).

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.

Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.

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.

c-Fms-IN-10, a derivative of thieno [3,2-d] pyrimidine, is a kinase inhibitor of FMS (Colony-stimulating factor-1 receptor, CSF-1R; IC50: 2 nM) with anti-tumor activity.

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.

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

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

JTE-952 is a oral, potent active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse

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).

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.

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

Enrupatinib is an inhibitor of the colony stimulating factor 1 receptor (CSF1R), exhibiting antitumor activity.

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.

cFMS Receptor Inhibitor II is a CSF1R kinase (FMS Receptor; colony stimulating factor 1 receptor; Macrophage colony-stimulating factor receptor) inhibitor with an IC50 of 2.8 nM, demonstrating significant selectivity over other kinases. This compound also exhibits notable CSF1R inhibition with an IC50 of 1.4 μM in cellular assays.

CSF1R-IN-13 is a powerful CSF1R inhibitor with potential applications in researching cancer diseases [1]. CSF1R, also known as colony stimulating factor 1 receptor, is a critical growth factor that regulates various cell types, including bone marrow progenitor cells, monocytes, macrophages, and giants [1]. CSF1R-IN-13 shows promise in furthering our understanding of cancer-related disorders (WO2019134661A1, compound 32) [1].

Edicotinib, also known as JNJ-40346527, is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tumor cells.

Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3 STK1), colony-stimulating factor 1 receptor (CSF1R FMS), stem cell factor receptor (SCFR KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases.