2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Fms c-Kit Apoptosis
  4. Pexidartinib hydrochloride

Pexidartinib hydrochloride  (Synonyms: PLX-3397 hydrochloride)

Cat. No.: HY-16749A Purity: 99.77%
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Pexidartinib hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.

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

CAS No. : 2040295-03-0

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Customer Review

Based on 144 publication(s) in Google Scholar

Other Forms of Pexidartinib hydrochloride:

Pexidartinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

144 Publications Citing Use of MCE Pexidartinib hydrochloride

In Vivo Efficacy Study
IF
WB
In Vivo Imaging
Cell Imaging/Staining
Cell Proliferation/Viability Assay

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

    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.

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

    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.

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

    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.

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

    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.

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

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

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

    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.

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

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

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

    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.

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

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

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

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

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

    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.

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

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pexidartinib hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity[1].

    IC50 & Target

    IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1]
    In Vitro

    Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Pexidartinib hydrochloride Related Antibodies
    In Vivo

    Pexidartinib hydrochloride can be used to deplete the microglia cells in mice.
    Pexidartinib (290 ppm in AIN-76A standard chow, 21 days) hydrochloride depletes the microglia cells in brain by 70% in adult male C57BL/6 J mice (20-25 g)[5].
    Pexidartinib (600 ppm in chow, 10 days and 30 days ) hydrochloride depletes the microglia cells more than 90% in brain of C57BL/6J mice[6].
    Pexidartinib hydrochloride (0.25, 1 mg/kg, i.p., twice daily for 8 days) hydrochloride inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2].
    Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) hydrochloride shows no obvious effect on the cleaved caspase-3-positive cells in mice[2].
    Pexidartinib hydrochloride (50 mg/kg; p.o.; every second day for 3 weeks) hydrochloride reduces tissue macrophage levels without affecting glucose homeostasis in mice[4].
    Pexidartinib hydrochloride has limited permeability to the blood-brain barrier, primarily through ABCB1[7].
    Pexidartinib hydrochloride can mainly penetrate the damaged blood-brain barrier surrounding the tumor, allowing tumor cells to enter the intact blood-brain barrier[8].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Neonatal mice[2]
    Dosage: 0.25, 1 mg/kg
    Administration: I.P. twice daily for 8 days
    Result: Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells.
    Animal Model: 10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice)[4]
    Dosage: 50 mg/kg
    Administration: P.o.; every second day for 3 weeks
    Result: Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels.
    Molecular Weight

    454.28

    Formula

    C20H16Cl2F3N5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 60 mg/mL (132.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2013 mL 11.0064 mL 22.0129 mL
    5 mM 0.4403 mL 2.2013 mL 4.4026 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

    V1

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.77%

    SDS (394 KB)

    COA (247 KB) HNMR (139 KB) RP-HPLC (169 KB) LCMS (105 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2013 mL 11.0064 mL 22.0129 mL 55.0321 mL
    5 mM 0.4403 mL 2.2013 mL 4.4026 mL 11.0064 mL
    10 mM 0.2201 mL 1.1006 mL 2.2013 mL 5.5032 mL
    15 mM 0.1468 mL 0.7338 mL 1.4675 mL 3.6688 mL
    20 mM 0.1101 mL 0.5503 mL 1.1006 mL 2.7516 mL
    25 mM 0.0881 mL 0.4403 mL 0.8805 mL 2.2013 mL
    30 mM 0.0734 mL 0.3669 mL 0.7338 mL 1.8344 mL
    40 mM 0.0550 mL 0.2752 mL 0.5503 mL 1.3758 mL
    50 mM 0.0440 mL 0.2201 mL 0.4403 mL 1.1006 mL
    60 mM 0.0367 mL 0.1834 mL 0.3669 mL 0.9172 mL
    80 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6879 mL
    100 mM 0.0220 mL 0.1101 mL 0.2201 mL 0.5503 mL
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    Pexidartinib hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Pexidartinib2040295-03-0PLX-3397PLX3397PLX 3397c-Fmsc-KitApoptosisCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RSCFRCD117Inhibitorinhibitorinhibit

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