Name | 6-(2,6-Dimethylphenyl)-2-{[4-(4-methyl-1-piperazinyl)phenyl]amino }pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one |
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Synonyms | Lck Inhibitor |
Description | 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: Lckin 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 μM·h (Cmax≈ 0.7 μM) [1].Clinical trial: N/A |
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Related Catalog | |
References |
Molecular Formula | C31H30N8O |
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Molecular Weight | 530.62300 |
Exact Mass | 530.25400 |
PSA | 83.59000 |
LogP | 4.76970 |
Storage condition | 2-8℃ |