An inhibitor of PI3Kδ (IC50 = 0.011 µM); selective for PI3Kδ over PI3Kα

Leniolisib – 1 mg

Brand:
Cayman
CAS:
1354690-24-6
Storage:
-20
UN-No:
Non-Hazardous - /

Leniolisib is an inhibitor of PI3Kδ (IC50 = 0.011 µM).{40219} It is selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = 0.244, 0.424, and 2.23 µM, respectively). It inhibits phosphorylation of the PI3K target Akt in Rat-1 fibroblasts expressing P13K p110δ with an IC50 value of 0.056 µM. Leniolisib inhibits the mixed lymphocyte reaction (MLR), indicating inhibition of allogeneic T cell activation, in isolated human peripheral blood mononuclear cells (PBMCs) and isolated mouse splenocytes (IC50s = 0.079 and 0.033 µM, respectively). It also inhibits PI3Kδ-dependent B cell activation and IgM-induced B cell proliferation in isolated mouse splenocytes. Leniolisib (3 and 10 mg/kg) reduces the production of rat anti-rat collagen antibodies, as well as reduces paw swelling and joint erosion in a rat model of collagen-induced arthritis.  

 

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SKU: 28078 - 1 mg Category:

Description

An inhibitor of PI3Kδ (IC50 = 0.011 µM); selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = 0.244, 0.424, and 2.23 µM, respectively); inhibits phosphorylation of Akt in Rat-1 fibroblasts expressing P13K p110δ (IC50 = 0.056 µM); inhibits the MLR in isolated human PBMCs and isolated mouse splenocytes (IC50s = 0.079 and 0.033 µM, respectively); reduces the production of rat anti-rat collagen antibodies, as well as reduces paw swelling and joint erosion in a rat model of collagen-induced arthritis at 3 and 10 mg/kg

Formal name: 1-[(3S)-3-[[5,6,7,8-tetrahydro-6-[6-methoxy-5-(trifluoromethyl)-3-pyridinyl]pyrido[4,3-d]pyrimidin-4-yl]amino]-1-pyrrolidinyl]-1-propanone

Synonyms:  CDZ 173

Molecular weight: 450.5

CAS: 1354690-24-6

Purity: ≥98% (mixture of rotamers)

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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