| Identification | Back Directory | [Name]
5-Pyrimidinecarboxamide, 4-[[(1R)-1,2-dimethylpropyl]amino]-2-[[4-[(methylsulfonyl)oxy]phenyl]amino]- | [CAS]
1430095-30-9 | [Synonyms]
JAK3-IN-9
5-Pyrimidinecarboxamide, 4-[[(1R)-1,2-dimethylpropyl]amino]-2-[[4-[(methylsulfonyl)oxy]phenyl]amino]- | [Molecular Formula]
C17H23N5O4S | [MOL File]
1430095-30-9.mol | [Molecular Weight]
393.46 |
| Hazard Information | Back Directory | [Uses]
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research[1]. | [in vivo]
JAK3-IN-9 (compound 11i) (Female Lewis rats; 3, 10 and 30 mg/kg; Oral gavage once daily for 20 days) can selectively inhibit JAK3 cytokine signaling in the primary cells[1].
JAK3-IN-9 (Male DBA1j of 8 to 12-weeks old mice; 1mg/kg, Intravenous injection, Single administration) shows high AUC of 2104 μg/ml, extends t1/2 to 2.56 h and good oral bioavailability of 48%[1].
JAK3-IN-9 (30 mg/kg; Oral gavage once daily for 20 days) suppress paw swelling in a dose-dependent manner with ED50 value of 10 mg/kg[1]. | Animal Model: | Male DBA1j (8 to 12-weeks old) mice; Female Lewis rats[1]. | | Dosage: | 1, 3, 10 and 30 mg/kg | | Administration: | I.V, Single administration; IG, once daily for 20 days. | | Result: | Showed anti-arthritis activity in the CIA mice model[1]. |
| [IC 50]
JAK3: 1.7 nM (IC50) | [References]
[1] Bahekar R, et al. Discovery of diaminopyrimidine-carboxamide derivatives as JAK3 inhibitors. Bioorg Chem. 2020 Jun;99:103851. DOI:10.1016/j.bioorg.2020.103851 |
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