JTE-952

Modify Date: 2024-01-10 15:05:45

JTE-952 Structure
JTE-952 structure
Common Name JTE-952
CAS Number 1255303-54-8 Molecular Weight 518.60
Density N/A Boiling Point N/A
Molecular Formula C30H34N2O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of JTE-952


JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis[1].

 Names

Name JTE-952

 JTE-952 Biological Activity

Description JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis[1].
Related Catalog
Target

IC50: 13 nM (CSF1R), 261 nM (TrkA)[1].

In Vivo JTE-952 (3 mg/kg, p.o. once-daily) treatment reduces the overall progression of the clinical score, including inflammation and bone erosion in mouse model of collagen-induced arthritis (CIA model)[1]. Animal Model: Mouse model of collagen-induced arthritis (CIA model)[1]. Dosage: 3 mg/kg. Administration: Oral once-daily. Result: Reduced the overall progression of the clinical score, including inflammation and bone erosion.
References

[1]. Ikegashira K, et al. Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. Bioorg Med Chem Lett. 2019 Apr 1;29(7):873-877.

 Chemical & Physical Properties

Molecular Formula C30H34N2O6
Molecular Weight 518.60