Description
A BTK inhibitor (IC50 = 0.5 nM); greater than 20-fold selective for BTK over a panel of 384 kinases; inhibits BCR stimulation-induced calcium flux in Ramos B cells (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively); inhibits by Fcγ receptor stimulation-induced TNF-α production in human PBMCs (IC50 = 3 nM); reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model at 30 mg/kg per day; reduces hind paw tibiotarsal joint bone resrption and inflammation in a CAIA mouse model at 5 and 20 mg/kg
Formal name: (2S,5R)-6-fluoro-5-[(3S)-3-(8-fluoro-1,4-dihydro-1-methyl-2,4-dioxo-3(2H)-quinazolinyl)-2-methylphenyl]-2,3,4,9-tetrahydro-2-(1-hydroxy-1-methylethyl)-1H-carbazole-8-carboxamide
Synonyms:
Molecular weight: 572.6
CAS: 1643368-58-4
Purity: ≥98%
Formulation: A crystalline solid
