csf1r-in-2

CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).

Axl/Mer/CSF1R-IN-2 (Comp 4) serves as an inhibitor for Axl, Mer, and CSF1R [1].

CSF1R-IN-26 (Compound III-1) is an inhibitor of CSF-1R with an IC50 of 20.07 nM. It promotes the polarization of M2 macrophages to M1 macrophages, inducing apoptosis in MC-38 cancer cells. CSF1R-IN-26 inhibits the activation of the AKT/ERK/STAT3 signaling pathways, remodels the tumor immune microenvironment, and exhibits antitumor activity in mouse models. In SD rats, CSF1R-IN-26 demonstrates favorable pharmacokinetic properties, with a half-life of 1.86 hours and an oral bioavailability of 79.22%.

CSF1R-IN-20 (compound 7a), a CSF-1R inhibitor, exhibits an IC 50 of 467 nM and effectively inhibits CSF-1R auto-phosphorylation [1].

CSF1R-IN-21 (compound 7e), a CSF-1R inhibitor, exhibits potent inhibition with an IC 50 of 31 nM and effectively blocks CSF-1R auto-phosphorylation. It is utilized in researching neurodegenerative diseases [1].

CSF1R-IN-22 (Compound C19), a potent orally administered CSF-1R selective inhibitor (IC50 <6 nM), significantly enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration. Moreover, it amplifies the anti-tumor immune responses in conjunction with anti-PD-1 and triggers apoptosis in tumor cells. Additionally, CSF1R-IN-22 effectively reprograms M2-like TAMs (tumor-associated macrophages) to an M1 phenotype, modulates the tumor microenvironment (TME) by fostering the recruitment of CD8+ T cells, and diminishes the presence of immunosuppressive Tregs and MDSCs [1].

CSF1R-IN-23 (Compound 7dri), a selective colony-stimulating factor-1 receptor (CSF1R) inhibitor, exhibits an IC50 of 36.1 nM. This compound acts as an antineuroinflammatory agent in a mouse model and is noted for its blood-brain barrier (BBB) permeability [1].

CSF1R-IN-24 (Example 134), an orally active inhibitor of CSF1R, effectively reduces the survival of human iPSC-derived microglia (hiPSC-MG).

CSF1R-IN-25 (compound 36) serves as an orally effective inhibitor of CSF1R, applicable in the research of cancer, inflammation, and neurodegeneration.

PLX5622 hemifumarate is a highly selective, blood-brain barrier-permeable, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and a Ki of 5.9 nM. It can be used to eliminate proliferating and specific microglia before and during disease progression and is applicable for inducing Alzheimer's disease models.

Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.