leniolisib(CDZ 173)

Catalog No.S8752

leniolisib(CDZ 173) Chemical Structure

Molecular Weight(MW): 450.46

Leniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.

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Biological Activity

Description Leniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
Targets
PI3Kδ [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
DNA-PK [1]
()
DNA-PK [1]
(Cell-free assay)
0.011 μM 0.244 μM 0.424 μM 0.88 μM 0.88 μM
In vitro

In vitro, CDZ173 inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells. CDZ173 showed no activity up to the highest test concentration when tested against CYP isoform assays (3A3, 2D9, 2D6, 2C9), a panel of ion channels (including hERG) and a protease panel. In a panel of 50 safety related targets (GPCRs, ion channels, transporters), CDZ173 only showed measurable activity for hPDE4D (IC50 = 4.7 μM) and 5HT2B (IC50 = 7.7 μM)[1].

In vivo

In vivo, CDZ173 inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner. After prophylactic or therapeutic dosing, CDZ173 potently inhibited antigen-specific antibody production and reduced disease symptoms in a rat collagen-induced arthritis model. CDZ173 is absorbed very quickly across species as can be seen by an early Tmax of the oral profiles. Whereas clearance is low to moderate in rats and monkeys, it was found that clearance in dogs is very low resulting in a very high exposure in blood. Plasma protein binding in dogs is very high (>99%) and the distribution of the compound is restricted into tissue (Vss = 0.3 L/kg)[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Adult male Lewis rats (LEW/Han/Hsd)
  • Formulation: 0.5% Tween80 and 0.5% Carboxymethyl-cellulose in Water
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.79 mM)
Ethanol 13 mg/mL (28.85 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.46
Formula

C21H25F3N6O2

CAS No. 1354690-24-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02859727 Recruiting Activated PI3Kdelta Syndrome (APDS); PASLI Disease Novartis Pharmaceuticals|Novartis September 8 2016 Phase 2|Phase 3
NCT02859727 Recruiting Activated PI3Kdelta Syndrome (APDS); PASLI Disease Novartis Pharmaceuticals|Novartis September 8 2016 Phase 2|Phase 3
NCT02775916 Completed Primary Sjögren''s Syndrome Novartis Pharmaceuticals|Novartis June 1 2016 Phase 2
NCT02775916 Completed Primary Sjögren''s Syndrome Novartis Pharmaceuticals|Novartis June 1 2016 Phase 2
NCT02435173 Recruiting Common Variable Immunodeficiency (CVID) More Specifically Activated PI3Kdelta Syndrome (APDS) p110delta-activating Mutation Causing Senescent T Cells|Lymphadenopathy and Immunodeficiency (PASLI) Novartis Pharmaceuticals|Novartis August 24 2015 Phase 2|Phase 3
NCT02435173 Recruiting Common Variable Immunodeficiency (CVID) More Specifically Activated PI3Kdelta Syndrome (APDS) p110delta-activating Mutation Causing Senescent T Cells|Lymphadenopathy and Immunodeficiency (PASLI) Novartis Pharmaceuticals|Novartis August 24 2015 Phase 2|Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID