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

Pexidartinib  (Synonyms: PLX-3397)

Cat. No.: HY-16749 Purity: 99.17%
COA Handling Instructions

Pexidartinib (PLX-3397) est un récepteur du facteur 1 stimulant des colonies (CSF1R ou M-CSFR) et un inhibiteur de c-Kit qui est puissant, actif par voie orale, sélectif et compétitif pour l'ATP, avec des IC50 de 20 et 10 nM, respectivement. Pexidartinib (PLX-3397) présente une sélectivité de 10 à 100 fois pour le c-Kit et le CSF1R par rapport à d'autres kinases apparentées. Pexidartinib (PLX-3397) induit l'apoptose cellulaire et a une activité anti-tumorale.

Pexidartinib (PLX-3397) ist ein potenter, oral aktiver, selektiver und ATP-kompetitiver colony stimulating factor 1 receptor (CSF1R or M-CSFR) und c-Kit-Inhibitor mit IC50s von 20 bzw. 10 nM. Pexidartinib (PLX-3397) weist gegenüber anderen verwandten Kinasen eine 10- bis 100-fache Selektivität für c-Kit und CSF1R auf. Pexidartinib (PLX-3397) induziert Zellapoptose und hat Anti-Tumor-Aktivität.

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.

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

Pexidartinib Chemical Structure

Pexidartinib Chemical Structure

CAS No. : 1029044-16-3

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Customer Review

Based on 71 publication(s) in Google Scholar

Other Forms of Pexidartinib:

Top Publications Citing Use of Products

69 Publications Citing Use of MCE Pexidartinib

IF

    Pexidartinib 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 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 (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[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 (PLX-3397) 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.

    In Vivo

    Pexidartinib (PLX3397; 0.25, 1 mg/kg, twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2].
    Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice[2].
    Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice[4].

    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.
    Clinical Trial
    Molecular Weight

    417.81

    Formula

    C20H15ClF3N5

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (239.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3934 mL 11.9672 mL 23.9343 mL
    5 mM 0.4787 mL 2.3934 mL 4.7869 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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 5 mg/mL (11.97 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    %
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    %
    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).
    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: 99.64%

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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 2.3934 mL 11.9672 mL 23.9343 mL 59.8358 mL
    5 mM 0.4787 mL 2.3934 mL 4.7869 mL 11.9672 mL
    10 mM 0.2393 mL 1.1967 mL 2.3934 mL 5.9836 mL
    15 mM 0.1596 mL 0.7978 mL 1.5956 mL 3.9891 mL
    20 mM 0.1197 mL 0.5984 mL 1.1967 mL 2.9918 mL
    25 mM 0.0957 mL 0.4787 mL 0.9574 mL 2.3934 mL
    30 mM 0.0798 mL 0.3989 mL 0.7978 mL 1.9945 mL
    40 mM 0.0598 mL 0.2992 mL 0.5984 mL 1.4959 mL
    50 mM 0.0479 mL 0.2393 mL 0.4787 mL 1.1967 mL
    60 mM 0.0399 mL 0.1995 mL 0.3989 mL 0.9973 mL
    80 mM 0.0299 mL 0.1496 mL 0.2992 mL 0.7479 mL
    100 mM 0.0239 mL 0.1197 mL 0.2393 mL 0.5984 mL
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    Pexidartinib 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.

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