Pexidartinib

SKU: orb1306449

Description

Pexidartinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1029044-16-3
• MW: 417.81
• Purity: 99.21%
• Formula: C₂₀H₁₅ClF₃N₅
• SMILES: FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1
• Target: c-Kit,CSF-1R,FLT,Apoptosis,c-Fms
• Solubility: DMSO:72.1 mg/mL (172.57 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:7.7 mg/mL (18.43 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  FLT3:160 nM|c-Kit:10 nM|CSF1R:20 nM
• In Vivo:
  In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C Ly6 g F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.
• In Vitro:
  In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively.

Storage & Handling

• Storage: 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

FLT3, Inhibitor, PLX 3397, PLX3397, PLX-3397, Kit, inhibit, CSF-1R, CSF-1 receptor, CSF1R, CD117, c-Fms, cFms, colony stimulating factor 1 receptor, cKit, c-Kit, Apoptosis, Pexidartinib, SCFR

Compound Identifiers

PubChem CID

25151352