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.

Quick View
JNJ-28312141

Catalog No. A12687
Quick View

添加到收藏
CSF1R 抑制剂

JNJ-28312141是一种口服活性CSF1R抑制剂（Colony-stimulating factor-1受体，CRF1R），也是一种FLT3抑制剂。CSF1R在许多肿瘤中表达，是巨噬细胞的生长因子并介导破骨细胞分化。JNJ-28312141代表一种在急性髓样白血病中以及在依赖CSF-1的巨噬细胞和破骨细胞有助于肿瘤生长和骨骼事件的环境中具有潜在治疗活性的新药物。了解更多

Bulk Inquiry Free Sample
Quick View
AZD7507

Catalog No. A16886
Quick View

添加到收藏
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

Bulk Inquiry
Quick View
PLX5622

Catalog No. A18888
Quick View

添加到收藏
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

Bulk Inquiry
Quick View
JTE-952

Catalog No. A18391
Quick View

添加到收藏
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

Bulk Inquiry
Quick View
c-Fms-IN-8

Catalog No. A18879
Quick View

添加到收藏
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. 了解更多

Bulk Inquiry
Quick View
Linifanib (ABT-869)

Catalog No. A10025
Quick View

添加到收藏
VEGFR/PDGFR 抑制剂

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。了解更多

Product Citations (1)

Bulk Inquiry
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
Quick View
OSI-930

Catalog No. A10679
Quick View

添加到收藏
c-Kit/VEGFR 抑制剂

OSI-930是Kit，KDR，Flt，CSF-1R，c-Raf和Lck的有效抑制剂，IC50分别为80 nM，9 nM，8 nM，15 nM，41 nM和22 nM。了解更多

Bulk Inquiry Free Sample
Quick View
Pazopanib (GW-786034)

Catalog No. A11518
Quick View

添加到收藏
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)

Bulk Inquiry Free Sample
- 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
Quick View
GW2580

Catalog No. A11959
Quick View

添加到收藏
CSF-1R 抑制剂

GW2580是cFMS激酶的小分子，ATP竞争性抑制剂。了解更多

Product Citations (2)

Bulk Inquiry Free Sample
- Ravikanth Maddipati, .et al. MYC controls metastatic heterogeneity in pancreatic cancer, bioRxiv, 2021, February 01
- Liu M, .et al. Metabolic rewiring of macrophages by CpG potentiates clearance of cancer cells and overcomes tumor-expressed CD47-mediated 'don't-eat-me' signal, Nat Immunol, 2019, Jan 21 PMID: 30664738
Quick View
Ki 20227

Catalog No. A11472
Quick View

添加到收藏
M-CSFR, CSF1R 抑制剂

Ki 20227是c-Fms酪氨酸激酶(M-CSFR,CSF1R)的抑制剂。了解更多

Product Citations (1)

Bulk Inquiry
- Wensheng Wang, .et al. Lymphatic endothelial cells produce M-CSF causing massive bone loss in mice, J Bone Miner Res, 2017, May; 32(5): 939-950 PMID: 28052488
Quick View
CEP-32496

Catalog No. A13772
Quick View

添加到收藏
Raf 抑制剂

CEP-32496是一种口服v-raf鼠肉瘤病毒癌基因同源物B1（B-raf）丝氨酸/苏氨酸蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

Bulk Inquiry Free Sample
Quick View
BLZ945

Catalog No. A15540
Quick View

添加到收藏
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

Bulk Inquiry Free Sample
Quick View
Pexidartinib (PLX3397)

Catalog No. A15520
Quick View

添加到收藏
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)

Bulk Inquiry Free Sample
- 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
Quick View
Edicotinib

Catalog No. A13008
Quick View

添加到收藏
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. 了解更多

Bulk Inquiry
Quick View
GENZ-882706

Catalog No. A12484
Quick View

添加到收藏
CSF-1R Inhibitor

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1. 了解更多

Bulk Inquiry