Ibrutinib CAS NO.936563-96-1

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Ibrutinib shows the potent irreversible inhibitory effectivity fBtk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM 13 nM, respectively. ^[1] Ibrutinib exhibits a significant dose-dependent time-dependent induction of cytotoxicity inonic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation antagonizes the ability of CLL cells to proliferate after TLR signaling. ^[2] A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM results in inhibition of TNFα, IL-1β IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM 3.9 nM, respectively. ^[3]