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Ibrutinib

产品编号 T1835 CAS 936563-96-1

别名: 伊布替尼, 依鲁替尼, PCI-32765

Ibrutinib (PCI-32765) 是一种不可逆的、选择性的 Btk 抑制剂，IC50=0.5 nM，它是一种 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。

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Ibrutinib, CAS 936563-96-1

规格	价格/CNY	货期
5 mg	￥ 488	现货
10 mg	￥ 788	现货
50 mg	￥ 1,995	现货
100 mg	￥ 3,187	现货
200 mg	￥ 4,290	现货
1 mL * 10 mM (in DMSO)	￥ 488	现货

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其他形式的 Ibrutinib:

Ibrutinib-d5
询价
Ibrutinib Racemate
询价

选择批次

纯度: 99.79%

纯度: 99.76%

纯度: 99.71%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
靶点活性	FGR:2.3 nM (cell free), BLK:0.5 nM (cell free), Brk:3.3 nM (cell free), BTK:0.5 nM (cell free), BMX:0.8 nM (cell free), CSK:2.3 nM (cell free)
体外活性	In DOHH2, a cell line in which the BCR pathway can be activated by stimulation with anti-IgG, Ibrutinib (PCI-32765) 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). Continuous exposure to 10 nM PCI-32765 for 18 h completely prevented up-regulation of the B-cell activation marker CD69. A 1-h pulse exposure to 10 nM PCI-32765 resulted in a similar level of CD69 inhibition in B cells [1]. PCI-32765 inhibited BCR-activated primary B cell proliferation (IC50: 8 nM). Following FcγR stimulation, PCI-32765 inhibited TNFα, IL-1β and IL-6 production in primary monocytes (IC50s: 2.6/0.5/3.9 nM). Following FcεRI stimulation of cultured human mast cells, PCI-32765 inhibited release of histamine, PGD(2), TNF-α, IL-8, and MCP-1 [2]. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 inhibits activation-induced proliferation of CLL cells in vitro and effectively blocks survival signals provided externally to CLL cells from the microenvironment [3].
体内活性	PCI-32765 (3.125, 12.5, or 50 mg/kg per day) markedly inhibited clinical arthritis scores. Partial and nearly complete elimination of clinical signs of the disease occurred after 9 to 11 d of treatment at dosages of 3.125 and 12.5 mg/kg per day, respectively. An oral single dose of PCI-32765 at 3.125 mg/kg per day resulted in partial Btk occupancy in splenocytes, and the maximally efficacious dose (12.5 mg/kg per day) was sufficient to fully occupy Btk for 12 h [1]. PCI-32765 dose-dependently and potently reversed arthritic inflammation in a therapeutic CIA model (ED50: 2.6 mg/kg/day). PCI-32765 also prevented clinical arthritis in CAIA models. In both models, infiltration of monocytes and macrophages into the synovium was completely inhibited [2].
激酶实验	In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1].
细胞实验	CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 °C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab′)2 (10 μg/mL) and T cells were stimulated with anti-CD3/CD28 coated beads at a 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 μM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1].
动物实验	ale DBA/1 mice were immunized with type II collagen plus Freund adjuvant and boosted 21 d later. On a rolling basis, as significant swelling appeared in at least one paw, mice were enrolled and randomized. PCI-32765 or dexamethasone (0.2 mg/kg) was administered orally once per day for 11 d. Arthritis scores (0–5) were assigned to the mice based on the degree and extent of paw swelling. Mouse anti-type II collagen antibody and total IgG levels were measured by ELISA. Female MRL/MpJ-Faslpr mice received PCI-32765 by oral gavage once per day from week 8 through week 20. Proteinuria was monitored weekly. At week 20, serum was collected and analyzed for BUN and mouse anti-dsDNA antibody levels. Kidney histology was scored according to established criteria (26). No drug-induced weight loss was observed at any of the dose levels tested. These studies were carried out at Boulder Biopath according to approved animal care protocols. Results are presented as the mean ± SEM. Statistical significance between groups were evaluated with repeated measures one-way ANOVA or one-way ANOVA using GraphPad Prism with Tukey or Bonferroni multicomparison posttest [1].

别名	伊布替尼, 依鲁替尼, PCI-32765
化合物与蛋白结合的复合物	C-Src in complex with ibrutinib
分子量	440.5
分子式	C25H24N6O2
CAS No.	936563-96-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 82 mg/mL (186.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2701 mL	11.3507 mL	22.7015 mL	56.7537 mL
	5 mM	0.454 mL	2.2701 mL	4.5403 mL	11.3507 mL
	10 mM	0.227 mL	1.1351 mL	2.2701 mL	5.6754 mL
	20 mM	0.1135 mL	0.5675 mL	1.1351 mL	2.8377 mL
	50 mM	0.0454 mL	0.227 mL	0.454 mL	1.1351 mL
	100 mM	0.0227 mL	0.1135 mL	0.227 mL	0.5675 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. 2. Chang BY, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115. 3. Herman SE, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011 Jun 9;117(23):6287-96.

文献引用

1. Guo W, Liang D, Wang P, et al. HIF-PH Encoded by EGLN1 Is a Potential Therapeutic Target for Chronic Lymphocytic Leukemia. Pharmaceuticals. 2022, 15(6): 734 2. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 3. Zhang Z, Zhou H, Gu W, et al.CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes.Nature Chemical Biology.2024: 1-11.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ibrutinib 936563-96-1 Angiogenesis PROTAC Tyrosine Kinase/Adaptors Tyrosine Kinases Src BTK Ligands for Target Protein for PROTAC inhibit PCI 32765 伊布替尼 Target Protein-binding Moiety PCI32765 Inhibitor 依鲁替尼 Btk Bruton tyrosine kinase PCI-32765 inhibitor

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Ibrutinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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