PLX5622

Catalog No.S8874 Batch:S887405

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Technical Data

Formula

C21H19F2N5O
Molecular Weight 395.41 CAS No. 1303420-67-8
Solubility (25°C)* In vitro DMSO 50 mg/mL (126.45 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

Animal Study:

[3]
  • Animal Models

    AQP1 mice

  • Dosages

    100 mg/kg

  • Administration

    o.g.

Selleck's PLX5622 has been cited by 8 publications

Engineering an inhibitor-resistant human CSF1R variant for microglia replacement [ J Exp Med, 2023, 220(3)e20220857] PubMed: 36584406
Microglial Galectin3 enhances endothelial metabolism and promotes pathological angiogenesis via Notch inhibition by competitively binding to Jag1 [ Cell Death Dis, 2023, 14(6):380] PubMed: 37369647
Microglial Galectin3 enhances endothelial metabolism and promotes pathological angiogenesis via Notch inhibition by competitively binding to Jag1 [ Cell Death Dis, 2023, 14(6):380] PubMed: 37369647
Microglia-Derived Spp1 Promotes Pathological Retinal Neovascularization via Activating Endothelial Kit/Akt/mTOR Signaling [ J Pers Med, 2023, 13(1)146] PubMed: 36675807
A novel histone deacetylase inhibitor-based approach to eliminate microglia and retain astrocyte properties in glial cell culture [ J Neurochem, 2022, 10.1111/jnc.15581] PubMed: 35092690
Distinguished Functions of Microglia in the Two Stages of Oxygen-Induced Retinopathy: A Novel Target in the Treatment of Ischemic Retinopathy [ Life (Basel), 2022, 12(10)1676] PubMed: 36295111
A Pro-inflammatory Stimulus Disrupts Hippocampal Plasticity and Learning via Microglial Activation and 25-Hydroxycholesterol [ J Neurosci, 2021, JN-RM-1502-21] PubMed: 34725187
Down-regulation of Aquaporin-1 mediates a microglial phenotype switch affecting glioma growth [ Exp Cell Res, 2020, 396(2):112323] PubMed: 33058832

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.