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

Pexidartinib (Synonyms: PLX-3397)

Cat. No.: HY-16749 Purity: 99.64%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 55 In-stock
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10 mg USD 70 In-stock
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50 mg USD 150 In-stock
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100 mg USD 190 In-stock
Estimated Time of Arrival: December 31
200 mg USD 260 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Pexidartinib:

Top Publications Citing Use of Products

    Pexidartinib purchased from MCE. Usage Cited in: J Neuroinflammation. 2020 Jan 23;17(1):31.

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

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    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].

    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].

    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.
    Clinical Trial
    Molecular Weight

    417.81

    Formula

    C₂₀H₁₅ClF₃N₅

    CAS No.

    1029044-16-3

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (11.97 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2393 mL 1.1967 mL 2.3934 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 0.5 mg/mL (1.20 mM); Clear solution

    • 2.

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

      Solubility: ≥ 0.5 mg/mL (1.20 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.5 mg/mL (1.20 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.64%

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    Keywords:

    PexidartinibPLX-3397PLX3397PLX 3397c-FmsApoptosisc-KitCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RSCFRCD117Inhibitorinhibitorinhibit

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