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
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Pexidartinib hydrochloride:

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  • Biological Activity

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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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Pexidartinib hydrochloride
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