Edicotinib

Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research[1][2].

Product Specifications

CAS Number

[1142363-52-7]

Product Name Alternative

JNJ-40346527; JNJ-527

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

C-Fms

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Edicotinib.html

Purity

99.68

Solubility

DMSO : 16.67 mg/mL (ultrasonic)

Smiles

O=C(C1=NC=C(C#N)N1)NC2=C(C3=CCC(C)(C)CC3)N=C(C(CC(C)(C)O4)CC4(C)C)C=C2

Molecular Formula

C27H35N5O2

Molecular Weight

461.60

Precautions

H302, H315, H319, H335

References & Citations

[1]Mancuso R, et al. CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice.Brain. 2019 Oct 1;142 (10) :3243-3264.|[2]Genovese MC, et al. Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.J Rheumatol. 2015 Oct;42 (10) :1752-60.