Leniolisib

An inhibitor of PI3Kδ

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库存: 现货

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1mg

￥1087.00

870.00

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5mg

￥1962.00

1570.00

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10mg

￥3162.00

2530.00

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50mg

￥10687.00

8550.00

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100mg

￥18700.00

14960.00

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货号: ajci23184
CAS: 1354690-24-6
别名: CDZ173
分子式: C??H??F?N?O?
分子量: 450.46
纯度: >98%
溶解度: DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 25 mg/ml,Ethanol: 20 mg/ml
储存: Store at -20°C
库存: 现货

Background

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

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[1].

Oral leniolisib lead to a dose-dependent reduction in PI3K/AKT pathway activity and resolve the immune dysregulation with normalization of circulating transitional and na?ve 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[1].

Reference:

[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