c-Fms Inhibitor

JNJ-28312141 hydrochloride is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC₅₀ of 0.69 nM. JNJ-28312141 hydrochloride inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC₅₀s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 hydrochloride exhibits anti-inflammatory activity in mouse arthritis model.

CSF1R-IN-25 (compound 36) is an orally effective CSF1R inhibitor. CSF1R-IN-25 can be used to study cancer, inflammation, and neurodegeneration.

CSF1R-IN-19 is a potent inhibitor of CSF1R. CSF1R-IN-19 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-19 has the potential for the research of cancer.

Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with K_ds of <0.1 μM.

Dovitinib-d₈ is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.

CSF1R-IN-8 (Compound 22) is a CSF-1R inhibitor with an IC₅₀ of 0.012 μM.

Pimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC₅₀ value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity.

CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC₅₀<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8⁺ T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8⁺ T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs.

CSF1R-IN-18 (Compdound 16t), para-aniline derivative, is a colony-stimulating factor 1 receptor (CSF1R) inhibitor. CSF1R-IN-18 can be used for the research of cancers, CNS-diseases and bone diseases.

PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC₅₀s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively).

CSF1R-IN-10 (Compound 48) is a CSF-1R inhibitor with an IC₅₀ of 0.005 μM.

Edicotinib hydrochloride is a potent, selective, brain penetrant and orally active?colony-stimulating factor-1 receptor (CSF-1R)?inhibitor with an IC₅₀ of 3.2 nM. Edicotinib hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC₅₀ values of 20 nM and 190 nM, respectively. Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research.

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC₅₀ values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.

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.

CSF1R-IN-21 (compound 7e) is a CSF-1R Inhibitor with an IC₅₀ value of 31 nM. CSF1R-IN-21 inhibits CSF-1R auto-phosphorylation and can be used for the research of neurodegenerative diseases .

c-Fms-IN-15 (compound 8g) is a potent inhibitor of FMS kinase, with the IC₅₀ of 563 nM.

PXB17 can inhibit CSF1R (IC₅₀ = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC.

c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC₅₀ of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC₅₀, > 1 μM). Used in the research of autoimmune diseases.

CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC₅₀ values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury.

CSF1R-IN-20 (compound 7a) is a CSF-1R Inhibitor with an IC₅₀ value of 467 nM. CSF1R-IN-20 inhibits CSF-1R auto-phosphorylation.