产品描述: Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment. |
靶点:
PI3Kδ:11 nM (IC50);PI3Kα:280 nM (IC50);PI3Kβ:480 nM (IC50);PI3Kγ:2.57 μM (IC50);DNA-PK:880 nM (IC50);DNA-PK; PI3K |
体外研究:
Expression of APDS mutant p110δ in cell lines and patient-derived lymphocytes lead to increased pathway activity, measured as phosphorylation of AKT or S6, which is suppressed by leniolisib in a concentration dependent way |
体内研究:
Oral leniolisib lead to a dose-dependent reduction in PI3K/AKT pathway activity and resolve the immune dysregulation with normalization of circulating transitional and naïve B cells and reduction in PD-1+CD4+ and senescent CD57+CD8+ T cells. After 12 weeks of treatment, all patients show amelioration of lymphoproliferation with lymph node sizes and spleen volumes reduced by 39% (mean, range 26-57%) and 40% (mean, range: 13-65%), respectively |
参考文献:
1. Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 0028-4793; 1533-4406 |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.22 ml |
11.1 ml |
22.2 ml |
5 mM |
0.444 ml |
2.22 ml |
4.44 ml |
10 mM |
0.222 ml |
1.11 ml |
2.22 ml |
50 mM |
0.044 ml |
0.222 ml |
0.444 ml |
|
注意: |
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