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white powder |
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C25H24N6O2 |
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440.5 |
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in stock |
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936563-96-1 |
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99.5% |
Introduction
PCI-32765 is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM. IC50 & Target: IC50: 0.5 nM (Btk) In Vitro: 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]. In Vivo: 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].
