Home Protein Tyrosine Kinase CSF-1R inhibitor PLX5622 For research use only.

PLX5622

PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.

PLX5622 Chemical Structure

PLX5622 Chemical Structure

CAS: 1303420-67-8

Selleck's PLX5622 has been cited by 7 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with PLX5622

Tocilizumab (anti-IL-6R)

PLX5622 and Tocilizumab combination treatment inhibits M2-microglia polarization in vitro and reduces the occurrence of brain metastases of A549-F3 cells in vivo.

Jin Y, et al. Signal Transduct Target Ther. 2022 Feb 23;7(1):52.

Sotuletinib (BLZ945)

PLX5622 and BLZ945 impair calyceal pruning, diminish astrocytic GFAP in the lateral, low-frequency region of MNTB, and elevate glycine transporter 2 (GLYT2) levels in mice.

Chokr SM, et al. Sci Rep. 2022 Nov 2;12(1):18521.

ARRY-382

PLX5622 removes microglia by binding to the receptor, while ARRY-382 hinders cell growth without killing microglia.

Soto-Diaz K, et al. Front Immunol. 2021 Nov 26;12:734349.

GW2580

PLX5622 and GW2580 (PLX6134) have been used to eliminate microglia and CSF-1-dependent macrophages in various research settings.

Han J, et al. Cell Mol Life Sci. 2022 Apr 2;79(4):219.

PLX5622 Related Products

Signaling Pathway

CSF-1R Signaling Pathways

CSF-1R Signaling Pathway

Choose Selective CSF-1R Inhibitors

Biological Activity

Description PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.
Targets
CSF-1R [1]
(Cell-free assay)		 FLT3 [1]
(Cell-free assay)		 KIT [1]
(Cell-free assay)		 AURKC [1]
(Cell-free assay)		 KDR [1]
(Cell-free assay)
0.016 μM 0.39 μM 0.86 μM 1 μM 1.1 μM
In vitro
In vitro

PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.
Experimental Result Images Methods Biomarkers Images PMID
Western blot NLRP3 / β-actin / Iba1 PrPres 32242284
IHC RML / NBH 29769333
Immunofluorescence Thio-S / AC / OC / Aβ42 Thioflavin S / TMEM119 / Iba1 PBS / MTX cortical microglia microglia elimination IBA1 31434879
In Vivo
In vivo

In vivo PLX5622 demonstrates desirable PK properties in mice, rats, dogs, and monkeys, with a brain penetrance of ~20%. PLX5622 has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. PLX5622 is a useful compound for investigating microglial dynamics. It allows for the sustained and specific elimination of microglia, preceding and during pathology development of Alzheimer’s disease (AD). Long-term PLX5622-mediated microglial depletion is highly robust, sustainable, and specific to the microglial compartment[1].
Animal Research Animal Models AQP1 mice
Dosages 100 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01329991 Completed
Rheumatoid Arthritis
Plexxikon
 May 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 395.41 Formula

C21H19F2N5O
CAS No. 1303420-67-8 SDF --
Smiles CC1=CC2=C(NC=C2CC3=C(N=C(C=C3)NCC4=C(N=CC(=C4)F)OC)F)N=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (199.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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