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Poseltinib

Names

[ CAS No. ]:
1353552-97-2

[ Name ]:
Poseltinib

Biological Activity

[Description]:

Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> BMX Kinase
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
Research Areas >> Metabolic Disease

[Target]

IC50: 1.95 nM (BTK)[1]


[References]

[1]. Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H26N6O3

[ Molecular Weight ]:
470.52

Related Compounds