TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC 50 : 1.5 nM) and inhibits only three additional kinases BLK , BMX ( IC 50 = 1.6 nM) and TXK with IC 50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site ( IC 50 : 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8 , IL-1β , MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies.
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