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Leniolisib

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Chemical Structure| 1354690-24-6 同义名 : CDZ173
CAS号 : 1354690-24-6
货号 : A389627
分子式 : C21H25F3N6O2
纯度 : 99%+
分子量 : 450.457
MDL号 : MFCD30470232
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(233.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:2.23 μM

  • p110β

    PI3Kβ, IC50:0.424 μM

  • p110α

    PI3Kα, IC50:0.244 μM

  • p110δ

    PI3Kδ, IC50:0.011 μM
描述 Leniolisib is a selective PI3Kδ inhibitor with IC50 values of 0.205, 0.087, 0.128, 0.064 and 0.05μM for PI3K wt, PI3K N334K, E525K, E1021K and C416R mutant, most commonly described in APDS (activated PI3Kδ syndrome). It led a selective PI3Kδ inhibitor, caused dose-dependent suppression of PI3Kδ pathway hyperactivation (measured as phosphorylation of AKT/S6) in cell lines ectopically expressing APDS-causative p110δ variants and in T-cell blasts derived from patients. Oral leniolisib led to a dose-dependent reduction in PI3K/AKT pathway activity assessed ex vivo and improved immune dysregulation. The elevated serum levels of CXCL13, CXCL10, IFNγ, and TNF in APDS patients were reduced by leniolisib treatment to levels measured in healthy volunteers. Also it improved lymphadenopathy, splenomegaly and cytopenias in APDS patients[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL
参考文献

[1]Rao VK, Webster S, et al. Effective "activated PI3Kδ syndrome"-targeted therapy with the PI3Kδ inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316.

[2]Hoegenauer K, Soldermann N, et al. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980.

[3]Rao VK, Webster S, Dalm VASH, Šedivá A, van Hagen PM, Holland S, Rosenzweig SD, Christ AD, Sloth B, Cabanski M, Joshi AD, de Buck S, Doucet J, Guerini D, Kalis C, Pylvaenaeinen I, Soldermann N, Kashyap A, Uzel G, Lenardo MJ, Patel DD, Lucas CL, Burkhart C. Effective "activated PI3Kδ syndrome"-targeted therapy with the PI3Kδ inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316. doi: 10.1182/blood-2017-08-801191. Epub 2017 Sep 29. PMID: 28972011; PMCID: PMC5701526.