PLX5622

Catalog No.S8874

For research use only.

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

PLX5622 Chemical Structure

CAS No. 1303420-67-8

Selleck's PLX5622 has been cited by 3 Publications

Purity & Quality Control

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
Assay
Methods Test Index PMID
Western blot NLRP3 / β-actin / Iba1 ; PrPres 32242284 29769333
IHC RML / NBH 29769333
Immunofluorescence Thio-S / AC / OC / Aβ42 ; Thioflavin S / TMEM119 / Iba1 ; PBS / MTX ; cortical microglia ; microglia elimination ; IBA1 31434879 30241479 31122677 33841088 32242284
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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 395.41
Formula

C21H19F2N5O

CAS No. 1303420-67-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC2=C(NC=C2CC3=C(N=C(C=C3)NCC4=C(N=CC(=C4)F)OC)F)N=C1

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01329991 Completed Drug: PLX5622|Drug: Placebo Rheumatoid Arthritis Plexxikon May 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PLX5622 | PLX5622 supplier | purchase PLX5622 | PLX5622 cost | PLX5622 manufacturer | order PLX5622 | PLX5622 distributor