Shelf life (days): 730.0
Formulation: A solid
Formal Name: (4R)-4-[3-[(1S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl]-2-pyrrolidinone
Purity: ≥95%
Formula Markup: C20H22ClFN6O2
Formula Weight: 432.9
CAS Number: 1426698-88-5
Notes: Parsaclisib is an inhibitor of PI3Kδ (IC50 = 1 nM).{72499} It is selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = >10,000 nM for all), as well as a panel of 192 additional kinases and a panel of 70 ion channels and transporters at 1 µM. Parsaclisib inhibits the proliferation of primary human B cells (IC50 = 0.2 nM) and the production of cytokines in memory T cells (IC50s = 0.2-1.5 nM). It also inhibits the differentiation of naïve isolated human T cells into Th1, Th2, or Th17 T helper cells. It inhibits the proliferation of JeKo-1, Mino, Rec-1, and JVM-2 lymphoma cells (IC50s = 50s = 2-8 nM). In vivo, parsaclisib (0.1-10 mg/kg) reduces intratumoral phosphorylation of Akt and tumor growth in a Pfeiffer mouse xenograft model. Parsaclisib (3 mg/kg) reduces proteinuria, lymphadenopathy, and the severity of skin lesions in an MRL/MpJ-Fas lpr mouse model of spontaneous systemic lupus erythematosus (SLE).{72500} It also reduces salivary levels of TNF superfamily member 13B (TNFSF13B), also known as B cell activating factor (BAFF), and plasma levels of anti-SS-related antigen A (anti-SSA) and anti-SSB autoantibodies in a NOD.ShiLtJ mouse model of Sjögren’s syndrome.
Deutsch
English
