Shelf life (days): 1460.0
Formulation: A crystalline solid
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
Purity: ≥98% (mixture of rotamers)
Formula Markup: C21H25F3N6O2
Formula Weight: 450.457649
CAS Number: 1354690-24-6
Notes: 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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