Home PI3K/Akt/mTOR PI3K inhibitor leniolisib (CDZ 173) For research use only.

leniolisib (CDZ 173)

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.

leniolisib (CDZ 173) Chemical Structure

leniolisib (CDZ 173) Chemical Structure

CAS: 1354690-24-6

Selleck's leniolisib (CDZ 173) has been cited by 1 publication

Purity & Quality Control

Batch: S875201 DMSO] 90 mg/mL] false] Ethanol] 13 mg/mL] false] Water] Insoluble] false Purity: 99.47%
99.47

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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)		 Click to View More Targets
0.011 μM 0.244 μM 0.424 μM 0.88 μM 0.88 μM
In vitro
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

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].
Animal Research Animal Models Adult male Lewis rats (LEW/Han/Hsd）
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05693129 Recruiting APDS Pharming Technologies B.V.|CMIC Co Ltd. Japan|Labcorp Central Laboratory|Fortrea|Aixial Group August 30 2023 Phase 3
NCT05438407 Recruiting APDS Pharming Technologies B.V.|CMIC Co Ltd. Japan|Labcorp Central Laboratory|Fortrea|Aixial Group February 1 2023 Phase 3
NCT02859727 Active not recruiting Activated PI3Kdelta Syndrome (APDS); PASLI Disease Pharming Technologies B.V. September 8 2016 Phase 2|Phase 3
NCT02435173 Completed Common Variable Immunodeficiency (CVID) APDS / PASLI Novartis Pharmaceuticals|Novartis August 24 2015 Phase 2|Phase 3

Chemical lnformation & Solubility

Molecular Weight 450.46 Formula

C21H25F3N6O2
CAS No. 1354690-24-6 SDF --
Smiles CCC(=O)N1CCC(C1)NC2=NC=NC3=C2CN(CC3)C4=CC(=C(N=C4)OC)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (199.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
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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.

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