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Ibrutinib

CAS No. : 936563-96-1

MCE 站：Ibrutinib

产品活性：Ibrutinib (PCI-32765) 是一种不可逆的选择性 Btk 抑制剂，IC₅₀ 值为 0.5 nM。Ibrutinib 可作为 Btk 配体，用于合成一系列 PROTAC 分子，如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞，浓度为 10 和 100?nM 时，分别降解 73% 和 89% Btk。

研究领域：Protein Tyrosine Kinase/RTK  |  PROTAC

作用靶点：Btk  |  Ligand for Target Protein for PROTAC

In Vitro: Ibrutinib (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).
Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC₅₀=8 nM). Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC₅₀=2.6, 0.5, 3.9 nM, respectively).
Ibrutinib binds C481 (Cysteine481) of BTK with an ideal IC₅₀ of 0.5?nM. Ibrutinib cannot form a covalent bond with the hydroxyl group of serine, C481S mutation increases the IC₅₀ against BTK-C481S phosphorylation from 2.2?nM to 1?μM.

In Vivo: Ibrutinib (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. Ibrutinib (PCI-32765) inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces renal disease and autoantibody production in MRL-Fas(lpr) mice. Ibrutinib (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. Ibrutinib (PCI-32765) dose-dependently and potently reverses arthritic inflammation in a therapeutic CIA model with an ED₅₀ of 2.6 mg/kg/day. Ibrutinib (PCI-32765) also prevents clinical arthritis in CAIA models.

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