Cat No:LP000112
Product Name:PCI-32765;Ibrutinib
CAS NO:936563-96-1
Purity: ≥99%
Solubility: In DMSO
Storage: -10°C
PCI-32765 selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC50=11 nM), phosphorylation of Btk’s physiological substrate PLCγ (IC50=29 nM), and phosphorylation of a further downstream kinase, ERK (IC50=13 nM)[1]. PCI-32765 inhibits BCR-activated primary B cell proliferation (IC50=8 nM). Following FcγR stimulation, PCI-32765 inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC50=2.6, 0.5, 3.9 nM, respectively)[3].
PCI-32765 (3.125-50 mg/kg, p.o.) reduces the level of circulating autoantibodies and completely suppresses disease in mice with collagen-induced arthritis. PCI-32765 inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. PCI-32765 (3.125-50 mg/kg, p.o.) reduces renal disease and autoantibody production in MRL-Fas(lpr) mice[1]. PCI-32765 (0.1 μM) inhibits activation-induced proliferation of CLL cells, induces selective cytotoxicity in B cells compared with T cells, but alters activation induced T-cell cytokine production[2]. PCI-32765 dose-dependently and potently reverses arthritic inflammation in a therapeutic CIA model with an ED50 of 2.6 mg/kg/day. PCI-32765 also prevents clinical arthritis in CAIA models[3].

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