Signaling Pathway

c-Fms

c-Fms

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c-FMS (CSF1R) is located at the cell plasma membrane. c-FMS (CSF1R) is the receptor for the ligand colony stimulating factor-1 (CSF1). CSF1R is an integral transmembrane glycoprotein that exhibits ligand-induced tyrosine-specific protein kinase activity, which triggers a signaling cascade eventually affecting transcription of CSF1-responsive genes. CSF1R tyrosine phosphorylation is induced upon binding of CSF1, leading to activation of Ras / Erk and class I-A phosphatidylinositol 3-kinase signaling pathways, which in turn activate the signal transducers and activators of transcription (STATs) pathways, specifically STAT1, STAT3, and STAT5. CSF1R activation by CSF1 results in increased growth, proliferation and differentiation.

c-Fms Inhibitors & Modulators (7)

Product Name Catalog No. Brief Description
BLZ945

HY-12768

BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM; >3200-fold higher than its affinity for other kinases.

c-FMS inhibitor

HY-13075

c-FMS inhibitor is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.

GW2580

HY-10917

GW2580 is an orally bioavailable inhibitor of c-FMS kinase; completely inhibited human cFMS kinase in vitro at 0.06 microM and was inactive against 26 other kinases.

Ki20227

HY-10408

Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.

OSI-930

HY-10204

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.

Pexidartinib

HY-16749

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

PLX647

HY-13838

PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.