PLX5622

Catalog No.S8874 Batch:S887404

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Technical Data

Formula

C21H19F2N5O
Molecular Weight 395.41 CAS No. 1303420-67-8
Solubility (25°C)* In vitro DMSO 79 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (12.65mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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 clarify; 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%. This compound has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. It 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 this compound-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.

References

  • https://www.nature.com/articles/s41467-019-11674-z#Sec25
  • https://pubmed.ncbi.nlm.nih.gov/31434879/
  • https://pubmed.ncbi.nlm.nih.gov/33058832/

Selleck's PLX5622 Has Been Cited by 15 Publications

Macrophages Mediate Mesoscale Brain Mechanical Homeostasis [ Adv Mater, 2025, e17493.] PubMed: 41251505
FOXO1-driven metabolic reprogramming of hematomal CD8+ T cells drives the expansion of perihematomal edema following intracerebral hemorrhage [ Cell Mol Immunol, 2025, 22(12):1629-1641] PubMed: 41238793
Targeting formyl peptide receptor 2 to suppress neuroinflammation in neuromyelitis optica spectrum disorder [ Theranostics, 2025, 15(10):4495-4506] PubMed: 40225578
Inhibition of Bruton's tyrosine kinase restricts neuroinflammation following intracerebral hemorrhage [ Theranostics, 2025, 15(2):494-508] PubMed: 39744694
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells [ Mol Ther, 2025, S1525-0016(25)00871-8] PubMed: 41232525
Integration and functionality of human iPSC-derived microglia in a chimeric mouse retinal model [ J Neuroinflammation, 2025, 22(1):53] PubMed: 40016767
CD22 blockade exacerbates neuroinflammation in Neuromyelitis optica spectrum disorder [ J Neuroinflammation, 2024, 21(1):313] PubMed: 39616380
CD22 blockade modulates microglia activity to suppress neuroinflammation following intracerebral hemorrhage [ Pharmacol Res, 2023, 196:106912] PubMed: 37696483
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

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Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.