leniolisib (CDZ 173)

Catalog No.S8752 Batch:S875201

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Technical Data

Formula

C21H25F3N6O2

Molecular Weight 450.46 CAS No. 1354690-24-6
Solubility (25°C)* In vitro DMSO 90 mg/mL (199.79 mM)
Ethanol 13 mg/mL (28.85 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)
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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 (from reference)

Animal Study:

[1]

  • Animal Models

    Adult male Lewis rats (LEW/Han/Hsd)

  • Dosages

    10 mg/kg

  • Administration

    p.o.

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

Phosphatidyl Inositol 3-Kinase (PI3K)-Inhibitor CDZ173 protects against LPS-induced osteolysis [ Front Pharmacol, 2022, 13:1021714] PubMed: 36686650

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.