Edicotinib

SKU: orb1308350

Description

Edicotinib (JNJ-527) is a brain-penetrant, oral CSF-1R inhibitor with selectivity over KIT and FLT3. It suppresses microglial proliferation and neurodegeneration, making it a valuable research tool for studying Alzheimer's disease and rheumatoid arthritis in both in vitro and in vivo models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1142363-52-7
• MW: 461.6
• Purity: 98.58% (May vary between batches)
• Formula: C₂₇H₃₅N₅O₂
• SMILES: CC1(C)CCC(=CC1)c1nc(ccc1NC(=O)c1ncc([nH]1)C#N)C1CC(C)(C)OC(C)(C)C1
• Target: CSF-1R,c-Fms,c-Kit,FLT
• Solubility: DMSO:2.31 mg/mL (5 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.17 mM)

Bioactivity

• Target IC50:
  FLT3:190 nM|CSF1R:3.2 nM|c-Kit:20 nM
• In Vivo:
  METHODS: ME7 mice were treated with JNJ-527 (3, 10, 30, 100 mg/kg, oral) for five consecutive days at 12 weeks post-induction (wpi), followed by a dose-response experiment to evaluate the potential of Edicotinib (JNJ-527) to block microglial proliferation in ME7-prion mice. RESULTS Edicotinib (JNJ-527) administered at 30 mg/kg significantly blocked microglial proliferation in ME7-prion mice without altering the population dynamics in the healthy brain.
• In Vitro:
  METHODS: N13 mouse microglial cell line was incubated with Edicotinib (JNJ-527) (0.1, 1, 10, 100, 1000 nM) for 30 min. We characterized the effects of the selective CSF1R inhibitor JNJ-527 on CSF1R activation in vitro. RESULTS Edicotinib (JNJ-527) resulted in a dose-dependent decrease in CSF1R activation and a reduction in ERK1 and ERK2 phosphorylation, with an IC50 of 18.6 nM for CSF1R and 22.5 nM for ERK1/2.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Edicotinib, expansion, FLT3, neurodegeneration, microglial, inhibit, kit, JNJ 40346527, JNJ 527, JNJ40346527, JNJ-40346527, JNJ527, JNJ-527, colony stimulating factor 1 receptor, cKit, c-Fms, cFms, CSF-1R, CSF1R, CSF-1 receptor, alzheimer's disease, arthritis, rheumatoid

Compound Identifiers

PubChem CID

25230468