Ibrutinib (936563-96-1) is a very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR). Ibrutinib also potently inhibits several other kinases including BLK, BMS, FGR, EGFR, and ITK. It is a clinically useful...
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Ibrutinib (936563-96-1) is a very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR). Ibrutinib also potently inhibits several other kinases including BLK, BMS, FGR, EGFR, and ITK. It is a clinically useful drug to treat B cell cancers. It inhibits CLL cell migration and survival and downregulates expression of CD20. It enhanced antitumor immune responses in combination with anti PD-L1 blockade via its inhibition of ITK (IL2-inducible T-cell kinase)
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BTK (Bruton tyrosine kinase), also known as tyrosine-protein kinase BTK, is a TEC-family non-receptor tyrosine kinase central to B-cell receptor signalling and B-lymphocyte development.
Biological function: Following B-cell receptor engagement, BTK is activated at the plasma membrane and phosphorylates PLCG2, promoting calcium mobilization and downstream protein kinase C signalling. This kinase activity is central to B-cell activation, differentiation and immune signalling.
