| Description | Lck Inhibitor is effective inhibitors of Lck (IC50: 7 nM). |
| In vitro | Lck Inhibitor 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 to day 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]. |
| molecular weight | 530.62 |
| Molecular formula | C31H30N8O |
| CAS | 847950-09-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (188.46 mM), Sonication is recommended. |
| References | 1. Martin, Matthew W.; Newcomb, John; Nunes, Joseph J.; et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of Medicinal Chemistry (2008), 51(6), 1637-1648. 2. Liew, Chin Y.; Ma, Xiao H.; Liu, Xianghui; Yap, Chun W. SVM Model for Virtual Screening of Lck Inhibitors. Journal of Chemical Information and Modeling (2009), 49(4), 877-885. |