You are here:Home-Chemical Inhibitors & Agonists-Tyrosine Kinase-c-Fms (CSF1R)

Request The Product List ofc-Fms (CSF1R) c-Fms (CSF1R)

Colony stimulating factor 1 receptor (CSF1R, c-Fms, CD115) is a tyrosine kinase transmembrane receptor for a cytokine called colony stimulating factor 1 (CSF-1). CSF-1R and its ligands, CSF-1 and interleukin 34 (IL-34), regulate the function and survival of tumor-associated macrophages, which are involved in tumorigenesis and in the suppression of antitumor immunity.

In solid tumors, targeting CSF-1R via either small molecules or antibodies has shown interesting results in vitro but limited antitumor activity in vivo. Blocking CSF-1/CSF-1R signaling represents a promising immunotherapy approach and several new potential combination therapies for future clinical testing.

PLX-3397 (pexidartinib) is an oral, potent, multi-target receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 and is the most advanced selective CSF-1R inhibitor under clinical development. ABT-869 (linifanib) is an oral inhibitor of CSF-1R tyrosine kinase conducted a phase II trial in which ABT869 was administered to patients with hepatocellular carcinoma. BLZ-945 is another orally active, bioavailable, potent, and selective inhibitor of CSF-1R, which is currently being assessed in a first-in-man phase I/II study as a single agent or in combination with PDR-001 (anti-PD-1 antibody) in several advanced solid tumors. Besides, multiple anti-CSF-1R monoclonal antibodies have also entered clinical trials, including FPA-008 (cabiralizumab), RG-7155 (RO5509554), IMC-CS4 (LY3022855) and AMG-820.

The development of new CSF-1R/CSF-1 axis inhibitors represents an attractive method for managing patients with metastatic solid tumors refractory to the standards of care or with diffuse/relapsed TGCT. Recent clinical trials testing CSF-1R inhibitors as monotherapies have shown encouraging results in the management of PVNS but disappointing outcomes for the treatment of solid tumors.



1. Peyraud F, et al. Curr Oncol Rep. 2017 Sep 5;19(11):70.

2. Pyonteck SM, et al. Nat Med. 2013 Oct;19(10):1264-72.

3. Kogan M, et al. Anticancer Res. 2012 Mar;32(3):893-9.

4. Albert DH, et al. Mol Cancer Ther. 2006 Apr;5(4):995-1006.


Cat. No. Product Name Information


CSF1R inhibitor

Vimseltinib (DCC-3014) is a potent, selective, orally active inhibitor of colony-stimulating factor 1 receptor (CSF1R/c-Fms), inhibits CSF1R phosphorylated juxtamembrane domain (JMD) with IC50 of 2.8 nM, 100-fold less potency against fully phosphorylated CSF1R (IC50=290 nM).


CSF1R inhibitor

RA03546849 (CSF1Rinh, GENZ-882706) is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.


CSF1R inhibitor

ARRY-382 (PF-07265804) is a highly potent, selective, oral inhibitor of CSF1R with an IC50 of 9 nM.


CSF1R inhibitor

JTE-952 (JTE952) is a potent, selective colony stimulating factor-1 receptor (CSF1R) type II inhibitor with IC50 of 14 nM, shows cellular activity in BMMCs IL-6 secretion assays with IC50 of 20 nM.


CSF1R inhibitor

AZD7507 (AZD-7507) is a potent, selective, orally available CSF-1R (c-FMS) with IC50 of 32 nM.

JNJ-28312141 hydrochloride

CSF1R inhibitor

JNJ-28312141 hydrochloride is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.


CSF1R inhibitor

JNJ-28312141 is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.


CSF1R inhibitor

c-FMS-IN-8 is a potent, selective c-FMS kinase inhibitor with IC50 of 0.8 nM, shows activity in collagen-induced model of arthritis in mice.


CSF1R inhibitor

Sotuletinib (BLZ945) is a potent, selective, brain-penetrant CSF-1R inhibitor with biochemical IC50 of 1 nM, displays >3,200-fold selectivity over other kinases (c-Kit, PDGFR-β, Flt3, Abl, etc.).


CSF1R inhibitor

CSF1R-IN-22 is a potent, cellular active and orally bioavailable CSF1R inhibitor with IC50 of 0.5 nM, displays 120-fold selectivity over c-Kit.


CSF1R inhibitor

PLX5622 (PLX-5622) is a potent, selective, orally active inhibitor of CSF1R tyrosine kinase (c-Fms) activity with Ki of 5.9 nM, 60-fold less potency against KIT.


CSF1R inhibitor

Edicotinib (JNJ-40346527, PRV 6527) is a potent, selective, orally bioavailable CSF-1R inhibitor with IC50 of 3.2 nM.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:

Copyright © 2022 All Rights Reserved. probechem Copyright

Contact Us