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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

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.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsCSF-1R

PLX5622

T71001303420-67-8

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

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Pexidartinib

T21151029044-16-3

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

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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.

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Edicotinib

T151991142363-52-7

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

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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.

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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).

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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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Vimseltinib

T106521628606-05-2

Vimseltinib (DCC-3014) is a dual inhibitor targeting c-FMS (CSF-IR) and c-Kit with IC50 values of less than 0.01 μM and 0.1-1 μM, respectively.

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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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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).

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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.

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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.

$108

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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.

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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.

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AZD7507

T143801041852-85-0

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

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Axatilimab

T769152155851-88-8

Axatilimab (SNDX-6352) is a human IgG4 antibody targeting the colony-stimulating factor 1 receptor (CSF-1R), which can be used for the study of immune system disorders and respiratory diseases.

$197

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Mavrilimumab

T766901085337-57-0

Mavrilimumab (CAM 3001) is a monoclonal antibody with antiviral activity that targets the α subunit of the granulocytic-macrophage colony-stimulating factor (GM-CSF) receptor, inhibiting downstream intracellular GM-CSF signaling. GM-CSF may contribute to an overactive inflammatory response linked to respiratory failure and death and could be used to study rheumatoid arthritis.