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-22914	ABSK021 CSF1R inhibitor	Pimicotinib (ABSK021) is a highly potent and selective, orally active inhibitor of CSF-1R, shows significant pre-clinical anti-tumor activity.
PC-38376	Vimseltinib 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).
PC-72412	RA03546849 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.
PC-38120	ARRY-382 CSF1R inhibitor	ARRY-382 (PF-07265804) is a highly potent, selective, oral inhibitor of CSF1R with an IC50 of 9 nM.
PC-36143	JTE-952 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.
PC-35232	AZD7507 CSF1R inhibitor	AZD7507 (AZD-7507) is a potent, selective, orally available CSF-1R (c-FMS) with IC50 of 32 nM.
PC-63412	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.
PC-63411	JNJ-28312141 CSF1R inhibitor	JNJ-28312141 is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.
PC-43376	c-FMS-IN-8 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.
PC-43194	BLZ945 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.).
PC-62826	CSF1R-IN-22 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.
PC-62741	PLX5622 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.

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