CSF-1R

Inhibitory Selectivity

Catalog No.	Inhibitor Name	CSF-1R	Other
A10025	Linifanib	***	VEGFR1/FLT1,FLT3,VEGFR2/KDR
A10679	OSI-930	**	FLT1,KDR,LCK
A11959	GW2580	*
A13772	CEP-32496	***	c-Kit,RET,PDGFRβ
A15520	Pexidartinib	**
A15540	BLZ945	****
A11472	Ki 20227	****	VEGFR-2, PDGFRβ, c-Kit

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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BLZ945

Catalog No. A15540
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CSF1R 抑制剂

BLZ945是有效的选择性CSF-1R激酶抑制剂。它减弱了TAM的周转率，同时增加了浸润宫颈癌和乳腺癌的CD8+ T细胞的数量。了解更多

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Pexidartinib (PLX3397)

Catalog No. A15520
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CSF1/Kit/FLT3 抑制剂

Pexidartinib (PLX3397)是KIT，CSF1R和FLT3的小分子酪氨酸激酶（RTK）抑制剂，具有潜在的抗肿瘤活性。了解更多

Product Citations (5)

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- Lu Luo, .et al. Intermittent theta-burst stimulation improves motor function by inhibiting neuronal pyroptosis and regulating microglial polarization via TLR4/NF κB/NLRP3 signaling pathway in cerebral ischemic mice, J Neuroinflammation, 2022, Jun 11;19(1):141 PMID: 35690810
- Sarah R Anderson,, .et al. Neuronal apoptosis drives remodeling states of microglia and shifts in survival pathway dependence, bioRxiv, 2022, 01.05.475126
- Hannah D Mason, .et al. Glia limitans superficialis oxidation and breakdown promotes cortical cell death after repeat head injury, JCI Insight, 2021, Oct 8;6(19):e149229 PMID: 34428178
- Chritica Lodder, .et al. CSF1R inhibition rescues tau pathology and neurodegeneration in an A/T/N model with combined AD pathologies, while preserving plaque associated microglia, Acta Neuropathol Commun, 2021, Jun 8;9(1):108 PMID: 34103079
- Anderson SR, .et al. Developmental Apoptosis Promotes a Disease-Related Gene Signature and Independence from CSF1R Signaling in Retinal Microglia, Cell Rep, 2019, May 14;27(7):2002-2013.e5 PMID: 31091440
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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

Product Citations (3)

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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AZD7507

Catalog No. A16886
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CSF-1R 抑制剂

AZD7507是一种有效的选择性CSF-1R抑制剂（32 nM细胞活性），AZD7507被认为是一种很有前途的化合物，因为它保留了AZ683所需的效能和口服药代动力学特性。了解更多

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PLX5622

Catalog No. A18888
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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. 了解更多

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JTE-952

Catalog No. A18391
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CSF-1R 抑制剂

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. 了解更多

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