c-Fms (CSF1R) (inhibitors, antagonists, agonists)-ProbeChem.com

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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.

References:

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
PC-61373	Edicotinib CSF1R inhibitor	Edicotinib (JNJ-40346527, PRV 6527) is a potent, selective, orally bioavailable CSF-1R inhibitor with IC50 of 3.2 nM.
PC-45069	Pexidartinib CSF1R inhibitor	Pexidartinib (PLX3397) is an oral-active, BBB-penatrant, potent mutil-targeted RTK inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively.
PC-42568	Ki20227 CSF1R inhibitor	Ki20227 is a potent, selective, orally active c-Fms inhibitor with IC50 of 2 nM.
PC-42737	GW2580 CSF1R inhibitor	GW2580 is a potent, selective c-Fms (CSF1R) inhibitor that completely inhibits human cFMS kinase in vitro at 60 nM.
PC-20762	CSF1R inhibitor 9 CSF1R inhibitor	CSF1R inhibitor 9 is a potent and highly selective purine-based inhibitor of CSF1R with enzymatic IC50 of 0.2 uM.
PC-73167	Elzovantinib MET/CSF1R/SRC inhibitor	Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively.

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