Product overview

Name Pexidartinib (PLX3397)
Purity >98%
Description

Potent CSF-1R inhibitor. Widely used microglia-depletion agent.

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Biological Data

Biological description

Potent CSF-1R inhibitor (IC50 = 20 nM). Reduces system and local macrophages accumulation without affecting Gr-1+ myeloid derived suppressor cells in the B16F10 mouse melanoma model. Promotes tumor growth control in combination with CD8 T-cell immunotherapy and improces adoptive cell therapy efficacy in the BRAFV600E-driven mouse melanoma model. Orally bioavailable. Recently reported to eliminate brain microglial temporarily and recoverably in adult mice.

Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in DMSO (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

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Dilution

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Chemical Data

Purity >98%
Chemical name N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
Molecular Weight 417.82
Chemical structure  Chemical Structure
Molecular Formula C20H15ClF3N5
CAS Number 1029044-16-3
PubChem identifier 25151352
SMILES C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F
InChi InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)
InChiKey JGWRKYUXBBNENE-UHFFFAOYSA-N
MDL number MFCD28900745

References for Pexidartinib (PLX3397)

References are publications that support the biological activity of the product
  • Pexidartinib (PLX3397) through restoring hippocampal synaptic plasticity ameliorates social isolation-induced mood disorders.

    Wang L et al (2022) International immunopharmacology 113 : 109436
  • Inhibition of Colony Stimulating Factor 1 Receptor Suppresses Neuroinflammation and Neonatal Hypoxic-Ischemic Brain Injury.

    Zhang B et al (2021) Frontiers in neurology 12 : 607370
  • Pexidartinib, a Novel Small Molecule CSF-1R Inhibitor in Use for Tenosynovial Giant Cell Tumor: A Systematic Review of Pre-Clinical and Clinical Development.

    Benner B et al (2020) Drug design, development and therapy 14 : 1693-1704

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