Formulation: A solid
Formal Name: N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide
Purity: ≥98%
Formula Markup: C26H26N6O3
Formula Weight: 470,5
Shelf life (days): 1460
CAS Number: 1353552-97-2
Notes: Poseltinib is an irreversible inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 1.95 nM).{31701} It is selective for BTK over a panel of 85 additional kinases at 2 µM but does inhibit the other Tec family kinases bone marrow tyrosine kinase on chromosome X (BMX), Tec, and TXK (IC50s = 0.64, 4.57, and 4.62 nM, respectively), as well as EGFR, Blk, and JAK3 (IC50s = 4.96, 13.5, and 14.6 nM, respectively). Poseltinib decreases the levels of CD40, CD69, or CD86 on primary human B cells activated with anti-IgM F(ab’)2 (IC50s = 4.2, 4.2, and 7.7 nM, respectively). It reduces the differentiation of isolated human CD14+ monocytes into osteoclasts when used at a concentration of 1 µM. Poseltinib (10 and 30 mg/kg) decreases disease severity and bone erosion in a mouse model of collagen-induced arthritis.
Deutsch
English
