Lck Inhibitor

847950-09-8

C31H30N8O

DMSO : 100 mg/mL (188.46 mM; Need ultrasonic)

Protein Tyrosine Kinase/RTK

Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM. IC50 Value: 7 nM [1] Target: Lck in vitro: Lck Inhibitor (compound 25) exhibited good potency in the T-cell receptor-induced IL-2 secretion assay (IL- 2) and also inhibited subsequent T-cell proliferation (T-cell prolif.) in the same human T -cells. in vivo: A once daily dose of 25was administered orally at 10, 30, and 60 mg/kg from day 9 today 17. Paw volume was measured daily from day 9 through day 18. The compound showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg (Figure 6). Based on the measured plasma levels from the three dose groups, the exposure of 25 at the ED50 was estimated to be 2.7 uM�h (Cmax? 0.7 uM) [1]. Clinical trial: N/A