Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR/PDGFR inhibitor
Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.
- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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M-CSFR, CSF1R inhibitor
Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).- Wensheng Wang, .et al. , J Bone Miner Res, 2017, May; 32(5): 939-950 PMID: 28052488
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VEGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. , Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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CSF-1R inhibitor
GW2580 is a small-molecule, ATP-competitive inhibitor of cFMS kinase.- Ravikanth Maddipati, .et al. , bioRxiv, 2021, February 01
- Liu M, .et al. , Nat Immunol, 2019, Jan 21 PMID: 30664738
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CSF-1R Inhibitor
GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1. -
CSF1R inhibitor
JNJ-28312141 is an orally active CSF1R inhibitor (Colony-stimulating factor-1 receptor, CRF1R) and also a FLT3 inhibitor. CSF1R is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. JNJ-28312141 represents a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth and skeletal events. -
CSF-1 receptor inhibitor
Edicotinib is a selective and orally available colony-stimulating factor-1 (CSF-1) receptor inhibitor, and has entered phase IIA clinical trial to study rheumatoid arthritis (RA) despite disease. -
CSF1/Kit/FLT3 inhibitor
Pexidartinib is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.- Haocheng Qin, .et al. , Research (Wash D C), 2025, Sep 11:8:0861 PMID: 40948936
- Hannah D Mason, .et al. , Nat Immunol, 2025, Jul;26(7):1152-1167 PMID: 40555833
- Sarah Vanherle, .et al. , Mol Psychiatry, 2025, Oct;30(10):4512-4528 PMID: 40307424
- Lu Luo, .et al. , J Neuroinflammation, 2022, Jun 11;19(1):141 PMID: 35690810
- Sarah R Anderson,, .et al. , bioRxiv, 2022, 01.05.475126
- Hannah D Mason, .et al. , JCI Insight, 2021, Oct 8;6(19):e149229 PMID: 34428178
- Chritica Lodder, .et al. , Acta Neuropathol Commun, 2021, Jun 8;9(1):108 PMID: 34103079
- Anderson SR, .et al. , Cell Rep, 2019, May 14;27(7):2002-2013.e5 PMID: 31091440
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CSF-1R inhibitor
TE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis. -
CSF-1R, c-FMS Type II inhibitor
c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM. -
CSF1R inhibitor
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development.- Sang Hwan Lee, .et al. , Brain, 2024, Aug 28:awae221 PMID: 39194073
- Ilija Brizic, .et al. , Research Square, 2024, October 3rd
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tyrosine kinase inhibitor
Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM. -
CSF1R/c-Kit Inhibitor
Pexidartinib hydrochloride is a potent, orally active inhibitor of the colony stimulating factor 1 receptor (CSF1R) and c-Kit, demonstrating ATP-competitive activity with IC50 values of 20 nM and 10 nM, respectively. This compound exhibits selective inhibition, with 10- to 100-fold potency over other related kinases. Pexidartinib hydrochloride promotes apoptosis in affected cells and exhibits significant anti-cancer properties, making it a valuable tool for research in oncology and immunology. -
FGFR1/2/3/ CSF-1R Inhibitor
Segigratinib hydrochloride is a selective inhibitor of FGFR1, FGFR2, FGFR3, and CSF-1R, exhibiting IC50 values of 0.5 nM, 1.3 nM, 3.6 nM, and 3.8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to target multiple receptors involved in tumor progression highlights its potential for therapeutic applications in oncology. -
CSF-1R Inhibitor
CSF1R-IN-22 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 value of less than 6 nM. This compound enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration, thereby amplifying anti-tumor immune responses, particularly in combination with anti-PD-1 therapies. CSF1R-IN-22 effectively reprograms M2-like tumor-associated macrophages (TAMs) to the M1 phenotype, reshaping the tumor microenvironment by increasing CD8+ T cell recruitment and decreasing immunosuppressive regulatory T cells and myeloid-derived suppressor cells (MDSCs). -
CSF-1R Inhibitor
Sotuletinib hydrochloride is a potent and selective inhibitor of the CSF-1R (c-Fms) with an IC50 value of 1 nM, demonstrating over 1,000-fold selectivity against related receptor tyrosine kinases. This orally bioavailable and brain-penetrant compound is utilized in research focused on microglia depletion, tumor biology, and central nervous system-related diseases, making it a valuable tool for advancing understanding in these areas. -
CSF1R Inhibitor
SYHA1813 is an inhibitor of the colony-stimulating factor 1 receptor (CSF1R) that demonstrates potent antitumor activity, particularly in glioblastoma (GBM). By targeting CSF1R, SYHA1813 modulates the tumor microenvironment and affects immune cell infiltration, making it a valuable tool for studying tumor progression and therapeutic resistance. This compound can be utilized in preclinical research to explore its efficacy in cancer treatment strategies. -
CSF1R Inhibitor
Enrupatinib is a selective inhibitor of colony-stimulating factor 1 receptor (CSF1R) with potent oral bioavailability and central nervous system (CNS) penetration. It effectively inhibits macrophage proliferation and osteoclast differentiation in vitro, thereby mitigating neuroinflammation and preserving neuronal integrity in Alzheimer's disease models. Enrupatinib has demonstrated the ability to reduce disease-associated microglia gene expression and enhance cognitive function in 5xFAD and J20 mouse models. Additionally, it attenuates tumor-associated macrophage infiltration and improves the antitumor efficacy of anti-PD-1 antibodies in preclinical models of colorectal and breast cancer, making it a valuable tool for research in these areas. -
CSF1R Inhibitor
AZ683 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R), with a high binding affinity (Ki=8 nM; IC50=6 nM). This compound demonstrates good oral bioavailability, making it suitable for in vivo studies. Additionally, [11C]AZ683 serves as a positron emission tomography (PET) radiotracer for visualizing CSF1R activity, enabling insights into its role in various biological processes and diseases. This compound is valuable for research applications focused on immune modulation and tumor microenvironment studies. -
CSF1R Inhibitor
CSF1R-IN-12 is a potent inhibitor of colony stimulating factor 1 receptor (CSF1R), which plays a crucial role in regulating bone marrow progenitor cells, monocytes, macrophages, and giant cells. By targeting CSF1R, this compound exhibits significant potential for cancer research, particularly in studies focused on the modulation of macrophage activity and tumor microenvironment interaction. CSF1R-IN-12 can aid in elucidating the role of CSF1R in various malignancies and in the development of novel therapeutic strategies. -
CSF1R Inhibitor
CSF1R-IN-24 is an orally active inhibitor of the colony-stimulating factor 1 receptor (CSF1R). This compound significantly reduces the survival of human induced pluripotent stem cell-derived microglia (hiPSC-MG), making it a valuable tool for studying microglial biology and potential therapeutic applications in neuroinflammatory conditions. Researchers can utilize CSF1R-IN-24 to investigate the role of microglia in various disease models and to explore new treatment strategies targeting the CSF1R pathway. -
CSF-1R Inhibitor
CSF1R-IN-3 is a potent and orally bioavailable inhibitor of the colony-stimulating factor 1 receptor (CSF-1R), with an IC50 of 2.1 nM. This compound exhibits significant antiproliferative activity against colorectal cancer cells by inhibiting the progression of the disease through the suppression of macrophage migration. Additionally, CSF1R-IN-3 facilitates the reprogramming of M2-like macrophages into the M1 phenotype, thereby enhancing antitumor immunity. This compound serves as a valuable tool for research in cancer immunology and macrophage biology. -
CSF1R/Mer/Axl Inhibitor
Adrixetinib is a potent triple inhibitor targeting CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM respectively. This compound serves as an effective immune modulator by remodeling the tumor microenvironment, enhancing the presence of M1 macrophages and CD8⁺ T cells while reducing M2 macrophages and myeloid-derived suppressor cells (MDSCs). Additionally, Adrixetinib increases the expression of MHC class I and E-cadherin in tumor cells, demonstrating significant antitumor efficacy in syngeneic mouse models. It is relevant for research involving breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma. -
CSF1R Inhibitor
BPR1R024 mesylate is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF1R), demonstrating potent inhibitory activity with an IC50 value of 0.53 nM. This compound is orally active and serves as a valuable tool for research in immuno-oncology, facilitating the exploration of CSF1R's role in tumor microenvironments and immune system modulation. BPR1R024 mesylate's targeted action enables detailed studies of its effects on macrophage biology and associated therapeutic strategies. -
PI3Kδ/CSF1R Inhibitor
JMC14 is a selective PI3Kδ and CSF1R inhibitor, exhibiting IC50 values of 12 nM and 143 nM, respectively. This compound preferentially disrupts PI3Kδ-mediated signaling within cells, demonstrating significant antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and in vivo models. JMC14 is an important tool for research into antitumor immunity and the mechanisms of cancer progression. -
CSF1-R Inhibitor
Sotuletinib dihydrochloride is a highly selective and potent inhibitor of the colony-stimulating factor 1 receptor (CSF1-R or c-Fms), exhibiting an IC50 of 1 nM and over 1,000-fold selectivity against closely related receptor tyrosine kinases. This compound is effective for the depletion of microglia and is valuable in research applications related to tumors and central nervous system (CNS) disorders. Its oral bioavailability and ability to penetrate the blood-brain barrier enhance its utility in neuropharmacological studies. -
Axl/Mer/CSF1R Inhibitor
Axl/Mer/CSF1R-IN-2 is a selective inhibitor targeting Axl, Mer, and CSF1R receptors. This compound demonstrates potent inhibition of these receptor kinases, which are implicated in various cancer types and immune response regulation. It is suitable for research applications focusing on tumor microenvironment modulation, immune checkpoint interactions, and potential therapeutic strategies in oncological studies. -
CSF1R Inhibitor
IACS-9439 is a potent and selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R) with a Ki value of 1 nM. This orally active compound demonstrates significant potential in cancer research, particularly for the treatment of advanced solid tumors. It enables investigation into the role of CSF1R in tumor microenvironments and immune modulation. -
CSF1R Inhibitor
CSF1R-IN-5 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R), which plays a critical role in the survival and differentiation of macrophages. By targeting the CSF-1/CSF-1R signaling pathway, CSF1R-IN-5 modulates the interaction between tumor-associated macrophages (TAMs) and glioma cells, influencing the exchange of inflammatory mediators. This compound is useful for research applications in cancer biology, particularly in studies investigating the tumor microenvironment and macrophage function in oncogenesis. -
CSF-1R Inhibitor
CSF1R-IN-7 is a selective inhibitor of Colony Stimulating Factor 1 Receptor (CSF-1R). This compound demonstrates potential in modulating microglial activation, making it a valuable tool for research in neuroinflammatory conditions such as Alzheimer’s disease. It is particularly useful for studying the role of CSF-1R in the pathology and progression of neurodegenerative disorders. -
CSF-1R Inhibitor
CSF1R-IN-9 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF-1R), demonstrating an IC50 of 0.028 μM. This compound effectively disrupts CSF-1R signaling, making it valuable for research on macrophage biology and inflammation. CSF1R-IN-9 can be utilized in investigating therapeutic strategies for conditions such as cancer and autoimmune diseases. -
CSF1R Inhibitor
CSF1R-IN-14 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF1R). As an isoindolinone derivative, it effectively modulates the activity of CSF-1, a key growth factor regulating the development and function of monocytes and macrophages. This compound holds potential for advancing research in cancer biology and studying immune responses associated with tumor progression. -
CSF1R Inhibitor
CSF1R-IN-23 is a selective inhibitor of colony-stimulating factor-1 receptor (CSF1R) with an IC50 of 36.1 nM. This compound demonstrates significant neuroinflammatory activity in mouse models, making it a valuable tool for studying neuroinflammation and related pathways. Additionally, CSF1R-IN-23 is permeable to the blood-brain barrier (BBB), facilitating its use in neurological research applications. -
CSF1R Inhibitor
CSF1R-IN-4 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R). This compound plays a critical role in modulating macrophage survival and differentiation by targeting the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 has been shown to influence the interaction between tumor-associated macrophages (TAMs) and glioma cells, making it a valuable tool for cancer research. Its potential applications include studying the tumor microenvironment and the immune response in various malignancies. -
CSF1R Inhibitor
CSF1R-IN-25 is a selective inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R). This compound demonstrates significant potential in modulating biological processes related to cancer, inflammation, and neurodegeneration. It serves as a valuable tool for researchers investigating the therapeutic implications of CSF1R inhibition in these areas. -
CSF1R Inhibitor
CSF1R-IN-19 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R). It modulates the interaction between tumor-associated macrophages and glioma cells, influencing the exchange of inflammatory factors. This compound is significant for cancer research, particularly in understanding the tumor microenvironment and exploring therapeutic strategies targeting CSF1R. -
Axl/Mer/CSF1R Inhibitor
Axl/Mer/CSF1R-IN-1 is an inhibitor of Axl/Mer receptor tyrosine kinases and CSF1R, demonstrating a binding affinity with Kds of less than 0.1 μM. This compound is valuable for research focused on the modulation of signaling pathways related to cancer, inflammation, and immune response. Its ability to precisely inhibit these targets makes it a useful tool in studies investigating the roles of Axl, Mer, and CSF1R in various biological processes. -
CSF-1R Inhibitor
CSF1R-IN-8 is a potent inhibitor of colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.012 μM. This compound exhibits significant biological activity in modulating CSF-1R signaling pathways, which are crucial for monocyte and macrophage differentiation and function. CSF1R-IN-8 is applicable in research focusing on immunology, cancer therapy, and the study of tumor microenvironments. -
CSF1R Inhibitor
CSF1R-IN-13 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF1R). As a crucial growth factor, CSF-1 modulates the development of bone marrow progenitor cells, monocytes, and macrophages, influencing immune response and cancer progression. This compound serves as a valuable research tool for investigating CSF1R's role in cancer therapies and related disease mechanisms. -
CSF-1R Inhibitor
CSF1R-IN-10 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.005 μM. This compound effectively disrupts CSF-1R signaling, which is crucial for the regulation of macrophage proliferation and differentiation. CSF1R-IN-10 is valuable for research applications focusing on inflammatory diseases, cancer, and the immune response, where modulation of macrophage activity is of interest. -
CSF-1R Inhibitor
Edicotinib hydrochloride is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF-1R), demonstrating an IC50 of 3.2 nM. This compound is brain penetrant and orally bioavailable, showing minimal off-target effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib hydrochloride effectively limits microglial expansion, attenuating neurodegeneration in preclinical models. Its unique profile offers potential applications in research related to Alzheimer's disease and rheumatoid arthritis. -
CSF1R Inhibitor
CSF1R-IN-21 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R) with an IC50 value of 31 nM. This compound effectively inhibits CSF1R auto-phosphorylation, making it a valuable tool for investigating the role of CSF1R in neurodegenerative diseases. CSF1R-IN-21 can be utilized in research studies aimed at understanding the molecular mechanisms underlying these conditions and exploring potential therapeutic interventions. -
CSF1R Inhibitor
CSF1R-IN-6 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R), which plays a critical role in regulating macrophage survival and differentiation through the CSF-1/CSF1R signaling pathway. This compound modulates the exchange of inflammatory mediators between tumor-associated macrophages (TAMs) and glioma cells, contributing to the understanding of tumor microenvironment interactions. CSF1R-IN-6 is a valuable tool for cancer research, particularly in elucidating the mechanisms underlying tumor progression and immune evasion. -
CSF-1R Inhibitor
CSF1R-IN-20 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF-1R), exhibiting an IC50 value of 467 nM. This compound effectively inhibits CSF-1R auto-phosphorylation, thereby interfering with downstream signaling pathways. It is primarily utilized in research applications focused on understanding macrophage biology and associated diseases, including cancer and inflammatory disorders.
