Description
A novel, irreversible, covalent second-generation BTK inhibitor with IC50 of 3nM; more potent and selective than ibrutinib, and does not inhibit EGFR, Itk or Txk; inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells; inhibits anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34mg/kg in mice; has promising safety and efficacy profiles for CLL treatment; orally active. Blood Cancer Approved