Leniolisib|1354690-24-6|(CDZ173)-陌孚医药/Medlife

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Leniolisib (Synonyms: CDZ173)

目录号: PL09833 纯度: ≥99%

CAS No. :1354690-24-6

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中文名称	Leniolisib
英文名称	Leniolisib
英文别名	Leniolisib;CDZ173;L22772Z9CP;(S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one;Leniolisib [INN];Leniolisib (CDZ173);Leniolisib (USAN/INN);CDZ173-NX;GTPL9424;MWKYMZXCGYXLPL-ZDUSSCGKSA-N;BDBM118299;SB18839;Example 67 [WO2012004299];1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d];Leniolisib free base;1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one;Cdz173 free base;Leniolisib; CDZ173;C
Cas No.	1354690-24-6
分子式	C₂₁H₂₅F₃N₆O₂
分子量	450.46
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Leniolisib (CDZ173)是高效，选择性的 PI3Kδ 抑制剂。Leniolisib 有潜力用于免疫缺陷类疾病的研究。

生物活性

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.

性状

Solid

IC50 & Target[1][2]

PI3Kδ 11 nM (IC50) PI3Kα 280 nM (IC50

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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

溶解度数据	In Vitro: DMSO : 100 mg/mL (222.00 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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