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CSF-1R

Colony stimulating factor 1 receptor (CSF1R), also known as macrophage colony-stimulating factor receptor (M-CSFR), and CD115 (Cluster of Differentiation 115), is a cell-surface protein encoded, in humans, by the CSF1R gene (known also as c-FMS). It is a receptor for a cytokine called colony stimulating factor 1.The encoded protein is a single pass type I membrane protein and acts as the receptor for colony stimulating factor 1, a cytokine which controls the production, differentiation, and function of macrophages. This receptor mediates most, if not all, of the biological effects of this cytokine. Ligand binding activates CSF1R through a process of oligomerization and trans-phosphorylation. The encoded protein is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases.

  • Edicotinib
    T151991142363-52-7
    Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
    • $64
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  • Pexidartinib
    T21151029044-16-3
    Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
    • $40
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  • PLX5622
    T71001303420-67-8
    PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor.
    • $97
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  • OSI-930
    T2624728033-96-3
    OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
    • $47
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  • Sotuletinib
    T6119953769-46-5
    Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.
    • $31
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  • Mavrilimumab
    T766901085337-57-0
    Mavrilimumab (CAM 3001) is a monoclonal antibody with antiviral activity that has an affinity for the α subunit of the granulocytic-macrophage colony-stimulating factor (GM-CSF) receptor and blocks downstream intracellular signaling of GM-CSF. GM-CSF may be associated with an overactive inflammatory response associated with respiratory failure and death, and could be used to study rheumatoid arthritis.
    • $289
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  • AZD7507
    T143801041852-85-0
    AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.
    • $84
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  • ARRY-382
    T353331313407-95-2
    ARRY-382 is a highly selective oral inhibitor of CSF-1R with an IC50 of 9 nM.
    • $117
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  • Linifanib
    T2514796967-16-3
    Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).
    • $43
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  • Ki20227
    T4315623142-96-1
    Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.
    • $39
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  • Vimseltinib
    T106521628606-05-2
    Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor (IC50s: <0.01 μM and 0.1-1 μM).
    • $84
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  • c-Fms-IN-8
    T106471255303-58-2
    c-Fms-IN-8 is a colony-stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor (IC50: 9.1 nM). It is compound 4a in the reference.
    • $1,400
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  • CSF1R-IN-3
    T640662760584-90-3
    CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC50 value of 2.1 nM. CSF1R-IN-3 has anti-proliferative activity against colorectal cancer cells. CSF1R-IN-3 exhibits anti-tumour effects and immune enhancing effects by inhibiting the migration of macrophages and inducing the reprogramming of M2-type macrophages to M1-type macrophages, thus exhibited activity against colorectal cancer cells.
    • $139
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  • Nampt-IN-1
    T43761698878-14-6
    Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
    • $33
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  • GENZ-882706
    T113902070864-35-4
    GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor.
    • $2,130
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  • Tandutinib
    T1667387867-13-2
    Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
    • $38
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  • PRN1371
    TQ00151802929-43-6
    PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).
    • $74
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  • Otilimab
    T771251638332-55-4
    Otilimab (GSK 3196165) is a humanized monoclonal antibody against granulocyt-macrophage colony-stimulating factor (GM-CSF). Otilimab has anti-inflammatory activity, regulates the biological function of GM-CSF by blocking the interaction between GM-CSF and its cell surface receptors, and can be used in studies to treat severe COVID-19 pneumonia.
    • $122
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