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JTE-952

Names

[ CAS No. ]:
1255303-54-8

[ Name ]:
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]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms

[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

Related Compounds