Pexidartinib hydrochloride

SKU: orb1687255

Description

Pexidartinib hydrochloride (PLX-3397 HCl) is an orally bioavailable, ATP-competitive inhibitor targeting CSF1R (IC50=20 nM) and c-Kit (IC50=10 nM). It induces apoptosis and is widely used in preclinical research to investigate tumor-associated macrophages and oncology in both in vitro and in vivo models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2040295-03-0
• MW: 454.28
• Purity: 99.88% (May vary between batches)
• Formula: C₂₀H₁₆Cl₂F₃N₅
• SMILES: Cl.FC(F)(F)C1=NC=C(C=C1)CNC2=NC=C(C=C2)CC3=CNC=4N=CC(Cl)=CC43
• Target: c-Kit,Apoptosis,c-Fms
• Solubility: H2O:< 1 mg/mL (insoluble);DMSO:48 mg/mL (105.66 mM)

Bioactivity

• Target IC50:
  FLT1:880 nM|KDR:350 nM|LCK:860 nM|cFMS:20 nM|NTRK3:890 nM|c-Kit:10 nM|FLT3:160 nM
• In Vivo:
  In the neonatal mouse model, Pexidartinib hydrochloride (0.25 and 1 mg/kg, intraperitoneal injection, twice daily for 8 days) inhibited the proliferation of microglia and BrdU-positive cells . Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 days) did not significantly affect the number of cleaved caspase-3-positive cells in mice . Pexidartinib hydrochloride (50 mg/kg, oral administration, once every two days for 3 weeks) reduced macrophage levels in mouse tissues without interfering with Vitis vinifera glucose homeostasis .
• In Vitro:
  Pexidartinib hydrochloride is a highly potent, selective, ATP-competitive inhibitor of CSF1R (cFMS) and c-Kit. It exhibits 10–100 times greater inhibitory selectivity for c-Kit and CSF1R compared to other related kinases (such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1), and NTRK3 (TRKC)), with IC50 values of 160 nM, 350 nM, 860 nM, 880 nM, and 890 nM, respectively .

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PLX3397 hydrochloride, PLX-3397 hydrochloride

Compound Identifiers

PubChem CID

73053710