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

Pexidartinib hydrochloride (Synonyms: PLX-3397 hydrochloride)

Cat. No.: HY-16749A Purity: 99.95%
Handling Instructions

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 exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Anti-cancer activity.

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

Pexidartinib hydrochloride Chemical Structure

Pexidartinib hydrochloride Chemical Structure

CAS No. : 2040295-03-0

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

Based on 7 publication(s) in Google Scholar

Other Forms of Pexidartinib hydrochloride:

Top Publications Citing Use of Products

    Pexidartinib hydrochloride 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

    • 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 exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. 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].

    In Vivo

    Pexidartinib (PLX3397; 0.25, 1 mg/kg, i.p., 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

    454.28

    Formula

    C₂₀H₁₆Cl₂F₃N₅

    CAS No.

    2040295-03-0

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

    DMSO : 60 mg/mL (132.08 mM; Need ultrasonic)

    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
    10 mM 0.2201 mL 1.1006 mL 2.2013 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: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    • 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

    • 3.

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

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

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

    Purity: 99.95%

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    Keywords:

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

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