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Pexidartinib

(Synonyms: PLX-3397)
161 Cited Publications
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Based on 161 publication(s) in Google Scholar

Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity. Pexidartinib has limited permeability to the blood-brain barrier, primarily through ABCB1.

For research use only. We do not sell to patients.

  • Purity: 99.56%
  • CAS No.: 1029044-16-3
  • Formula: C20H15ClF3N5
  • Molecular Weight:417.81
  • Storage:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Pexidartinib Chemical Structure
    Pexidartinib Chemical Structure
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
  • Experimental Validation Results for Pexidartinib
CAS No.: 1029044-16-3
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  • Pexidartinib Chemical Structure
    Pexidartinib Chemical Structure
    1/16
  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]

    Customer Validation
     Pexidartinib hydrochloride (0.01, 0.05, 0.1， 0.5, 1, 5, 10, 20 μM; 24 h) decreased the expression of p-Y719-KIT and increased the expression of cleaved PARP1 in a dose-dependent manner in WaGa cells.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Jul 1;10(15):e184465. [Abstract]

    Customer Validation
     PLX3397 groups were fed a diet containing Pexidartinib hydrochloride (PLX3397; 1,200 ppm) for 7 days starting at weaning (p21) and maintained for 7 days before analysis at 4-weeks of age (P28). (A&B) Representative images of retina cryo-sections stained for Iba1 and GFAP, respectively. (C) Representative merged images of CD31 and Iba1 staining of retina whole mounts in IgG and APB5-treated mice with or without administration of PLX3397.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Jul 1;10(15):e184465. [Abstract]

    Customer Validation
     PLX3397 groups were fed a diet containing Pexidartinib hydrochloride (PLX3397; 1,200 ppm) for 7 days starting at weaning (p21) and maintained for 7 days before analysis at 4-weeks of age (P28). Fluorescein angiographic images.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2025 Jan 2;32(1):86-104.e7. [Abstract]

    Customer Validation
     PLX3397 was incorporated into AIN-76A chow at a concentration of 400 mg/kg. Chimeric mice were fed either a control AIN-76A chow for 8 months, or fed control AIN-76A chow for 4 months and then PLX chow for 4 months. Representative images of microglia (Iba1, red) in the hippocampus of chimeric mice of each condition were shown. Scale bar, 500 μm.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Nov 13;41(11):1911-1926.e8. [Abstract]

    Customer Validation
     PLX-3397 was administered orally at 50 mg/kg every day beginning on the day before the first antibody administration.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 May;24(5):827-840. [Abstract]

    Customer Validation
     100 mg per kg body weight of pexidartinib was injected i.p. 24 and 48 h after DT injection. Representative histograms of EdU levels in lung extravascular CD64+ cells from DT-treated IMDTR mice that were treated with DT i.p. 3 days before, with the Csf1r antagonist PLX-3397 or with vehicle i.p. 1 and 2 days before, and with EdU i.p. 8 h before.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Feb 25;20(1):51. [Abstract]

    Customer Validation
     Pexidartinib (PLX3397; 290 mg/kg; in animal feedings; for 3 weeks) significantly decreases Iba-1 immunoreactive area in the mouse brains.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]

    Customer Validation
     PLX-3397 decreases Iba-1 expression, but has no impact on GFAP expression, in primary cultures of astrocytes. (A) Representative immunoblots of GFAP, Iba-1 and GAPDH with no exposure (−) and exposure to 0.2 µm, 1 µm and 5 µM Pexidartinib hydrochloride (PLX-3397; 17 days). Densitometric analysis of (B) Iba-1 and (C) GFAP was performed with ImageJ software using GAPDH as loading control.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]

    Customer Validation
     Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 17 days) decreased the percentage of Iba-1-expressing cells in primary cultures of astrocytes.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]

    Customer Validation
     Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 10, 17 days) did not compromise the viability of cultured astrocytes.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]

    Customer Validation
     Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 17 days) decreases the reactivity of cultured astrocytes. (A) Representative immunoblots of C3, PTX3 and GAPDH with no exposure (−) and exposure to 0.2 µm, 1 µm and 5 µM of PLX-3397. Densitometric analysis of (B) C3 and (C) PTX3 was performed with ImageJ software using GAPDH as loading control.

  • 1/16

    Pexidartinib purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2020 Jan 23;17(1):31. [Abstract]

    Customer Validation
     Representative Iba-1 immunofluorescent staining from the cortex and hippocampus in control and PLX3397-treated mice.

  • Pexidartinib