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

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.

Edicotinib（JNJ-40346527）is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity.

GW2580 is a selective inhibitor of human c-FMS with IC50 of 30 nM.

JNJ-28312141 is an orally active CSF1R inhibitor (Colony-stimulating factor-1 receptor, CRF1R) and also a FLT3 inhibitor.

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/PDGFR_beta_(IC50=451/217 nM), respectively.

PLX3397 is a tyrosine kinase inhibitor that potently inhibits the colony stimulating factor 1 (CSF1) receptor kinase, a driving force in the development and growth of PVNS.

DCC-3014(Vimseltinib) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.

ARRY-382 is a potent, oral and highly selective inhibitor of CSF1R/c-Fms with an IC50 of 9 nM. ARRY-382 can be used for the research of advanced or metastatic cancers.

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

TPX-0022 (CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.

c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively.

c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM.

BPR1R024 is an orally active and selective CSF1R inhibitor with IC50 of 0.53 nM. BPR1R024 specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth.

CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.

CSF1R-IN-5 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-5 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-5 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 11).

CSF1R-IN-4 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 104).

sCSF1Rinh is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.is highly selective for CSF1R as compared to other kinases with a selectivity score of S(35)=0.005, sCSF1Rinh exhibited excellent pharmacokinetic properties including good oral bioavailability and CNS penetrance.sCSF1Rinh (500 nM) blocks these phosphorylation events in CSF1 (100 ng/mL) stimulation of BV2 microglia.sCSF1Rinh inhibited murine bone marrow-derived macrophage proliferation with IC50 of 22 nM, sCSF1Rinh significantly depletes microglia in a concentration-dependent manner in murine mixed glial cultures (IC50=188 nM).sCSF1Rinh reduced the number of microglia and infiltrating macrophages in an acute LPS model, with diminished microglial/macrophage proliferation and attenuated inflammatory response.sCSF1Rinh also suppressed a deleterious microglial response in the C57BL/6 EAE (experimental autoimmune encephalomy) model as well as the MOG peptide-induced non-obese diabetic EAE model of progressive MS (NOD-EAE) and improved neurological impairments in both models.

Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.

BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.