Poseltinib

  • Chemical Properties
CAS No. 1353562-97-2 Cat. No. BCP29076
Name Poseltinib
Synonyms HM 71224; HM-71224; HM71224; LY 3337641; LY3337641; LY-3337641;
Formula C26H26N6O3 M. Wt 470.533
  • Biological Activity
Description Poseltinib, also known HM-71224 and LY3337641, is a tyrosine kinase inhibitor. Poseltinib is an experimental Bruton's tyrosine kinase inhibitor for the treatment of rheumatoid arthritis. HM71224 irreversibly bound to and inhibited Btk (IC50 = 1.95 nM). The compound also inhibited the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells and primary human B cells in a dose-dependent manner. Furthermore, HM71224 effectively inhibited the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes. HM71224 inhibits Btk in B cells and monocytes and ameliorates experimental arthritis in a mouse model. HM71224 is a potential novel therapeutic agent for rheumatoid arthritis in humans.
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets BTK 

Structure

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