| Bioactivity | 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]. |
| Target | IC50: 13 nM (CSF1R), 261 nM (TrkA). |
| 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: |
| Name | JTE-952 |
| CAS | 1255303-54-8 |
| Formula | C30H34N2O6 |
| Molar Mass | 518.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |