Poseltinib
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 |
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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