S82962 |
Leniolisib |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)