leniolisib (CDZ 173) - 99%, high purity , PI3-kinase p110-delta subunit inhibitor, CAS No.1354690-24-6, PI3-kinase p110-delta subunit inhibitor

Item Number

L414153

• Synonyms: Q27282602 | US8653092, 67 | Example 67 [WO2012004299] | Leniolisib | Leniolisib; CDZ173 | DC22326 | GTPL9424 | Leniolisib (USAN/INN) | LENIOLISIB [WHO-DD] | s8752 | (S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]p
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: PI3-kinase p110-delta subunit inhibitor

Product Description

Information

Leniolisib (CDZ 173) is a potentPI3Kδselective inhibitor withbiochemical IC50 valuesof 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.

Targets

PI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kβ (Cell-free assay); DNA-PK ; DNA-PK (Cell-free assay) 31052,0.011 μM; 0.244 μM; 0.424

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).

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).