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/ BTK / Ibrutinib/伊布替尼

Ibrutinib/伊布替尼 {[allProObj[0].p_purity_real_show]}

货号：A150396 同义名： 依鲁替尼 / PCI-32765; Imbruvica

Ibrutinib（PCI-32765）是一种选择性、不可逆的Btk抑制剂，IC50为0.5 nM。

Ibrutinib/伊布替尼 化学结构 CAS号：936563-96-1
Ibrutinib/伊布替尼 化学结构
CAS号：936563-96-1
Ibrutinib/伊布替尼 3D分子结构
CAS号：936563-96-1
Ibrutinib/伊布替尼 化学结构 CAS号：936563-96-1
Ibrutinib/伊布替尼 3D分子结构 CAS号：936563-96-1
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Ibrutinib/伊布替尼 纯度/质量文件 产品仅供科研

货号：A150396 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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产品名称 BTK ↓ 其他靶点 纯度
CGI-1746 +++

BTK, IC50: 1.9 nM

 		98%
Spebrutinib ++++

BTK, IC50: <0.5 nM

 		98+%
Acalabrutinib ++

BTK, IC50: 3nM

 		98%
CNX-774 +++

BTK, IC50: <1 nM

 		99%+
Ibrutinib ++++

BTK, IC50: 0.5 nM

 		98%
ONO-4059 analog +

BTK, IC50: 23.9 nM

 		98%
RN486 ++

BTK, IC50: 4 nM

 		99%+
(Z)-LFM-A13 +

BTK, Ki: 1.4 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ibrutinib/伊布替尼 生物活性

靶点

  • BTK

    BTK, IC50:0.5 nM
描述 Btk (Bruton tyrosine kinase), a non-receptor tyrosine kinase, is specifically required for BCR signaling which contributes to the initiation and maintenance of B-cell malignancies and autoimmune diseases. Ibrutinib, also called as PCI-32765 or imbruvica, is a potent Btk inhibitor with IC50 of 0.5 nM (measured by 33P filtration binding assay), modestly potent to Blk (IC50= 0.5 nM), Bmx (IC50= 0.8 nM), CSK (IC50= 2.3 nM), FGR (IC50= 2.3 nM), BRK (IC50= 3.3 nM), HCK (IC50= 3.7 nM), less potent to EGFR (IC50= 5.6 nM), Yes (IC50= 6.5 nM), ErbB2 (IC50= 9.4 nM), ITK (IC50= 10.7 nM). Ibrutinib can selectively inhibit B-cell signaling and activation, including inhibition of autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ and phosphorylation of a further downstream kinase ERK, in DOHH2 cells. Continuous exposure to 10 nM Ibrutinib for 18h completely prevented up-regulation of CD69, the B-cell activation marker. In vivo study shows that Btk inhibition by Ibrutinib is efficacious for autoimmune disease animal model. Oral treatment daily for 11 days with 12.5 mg/kg of Ibrutinib can inhibit collagen-induced arthritis in mice[1]. Up to now, Ibrutinib is approved to the treatment of mantle cell lymphoma, chronic lymphocytic leukemia, Waldenstrom's macroglobulinemia, small lymphocytic lymphoma, marginal zone lymphoma, and chronic graft versus host disease[2].
作用机制 Ibrutinib can bind covalently to a cysteine residue (Cys-481) in the active site, leading to potent and irreversible inhibition of Btk enzymatic activity[3]. Notice: BMX, EGFR, ErbB2, ITK, JAK3,AK3 and TEC is the kinase that contains a cysteine residue aligning with Cys-481 same as Btk, resulting in the binding with Ibrutinib[1].

Ibrutinib/伊布替尼 细胞实验

Cell Line
Concentration Treated Time Description References
Human embryonic stem cell (hESC)-derived ventricular cardiomyocytes 0.1, 0.5, 1.0 μM 30 minutes To evaluate the electrophysiological effects of ibrutinib on ventricular cardiomyocytes, showing no significant effects Stem Cell Reports. 2019 May 14;12(5):996-1006.
HL60/Adr 5 μM 72 hours To evaluate the reversal effect of PCI 29732 on MRP1-mediated multidrug resistance, results showed that PCI 29732 significantly enhanced the cytotoxicity of MRP1 substrate drugs Br J Pharmacol. 2014 Dec;171(24):5845-57.
HEK293/MRP1 5 μM 72 hours To evaluate the reversal effect of PCI 29732 on MRP1-mediated multidrug resistance, results showed that PCI 29732 significantly enhanced the cytotoxicity of MRP1 substrate drugs Br J Pharmacol. 2014 Dec;171(24):5845-57.
Human MDSC 1 μM 1 hour Ibrutinib treatment resulted in a decrease in the level of p-BTK. Cancer Res. 2016 Apr 15;76(8):2125-36.
human chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell lines 1 μM enhanced AID expression and translocation frequency Nature. 2017 Feb 23;542(7642):489-493.
mouse B cells 1 μM enhanced AID expression, increased somatic hypermutation (SHM) and chromosomal translocation frequency Nature. 2017 Feb 23;542(7642):489-493.
MSC2 cells 0.01 μM to 1 μM 1 hour Inhibited BTK phosphorylation, even at the 0.01 μM dose in the presence or absence of LPS stimulation. Cancer Res. 2016 Apr 15;76(8):2125-36.
U87 cells 0, 5, 10 μM 10 days Ibrutinib inhibited the proliferation and migration of LN229 and U87 cells, and induced apoptosis and autophagy. J Exp Clin Cancer Res. 2017 Jul 17;36(1):96.
LN229 cells 0, 5, 10 μM 10 days Ibrutinib inhibited the proliferation and migration of LN229 and U87 cells, and induced apoptosis and autophagy. J Exp Clin Cancer Res. 2017 Jul 17;36(1):96.
Primary microglial cells 1 μM 30 min Ibrutinib significantly downregulated the LPS-mediated increases in the levels of the mRNAs encoding the proinflammatory cytokines COX-2 and IL-6. J Neuroinflammation. 2018 Sep 19;15(1):271.
BV2 microglial cells 1 μM 30 min Ibrutinib significantly reduced LPS-induced increases in proinflammatory cytokine levels and regulated TLR4 signaling, decreasing p-AKT and p-STAT3 levels, suggesting that ibrutinib attenuates LPS-induced neuroinflammatory responses by inhibiting AKT/STAT3 signaling pathways. J Neuroinflammation. 2018 Sep 19;15(1):271.
DU145 cells 10 µM 72 h To evaluate the effect of CGI-1746 on prostate cancer cell survival, results showed that CGI-1746 was less effective at killing cells compared to irreversible BTK inhibitors at the same drug concentration. Cancer Biol Ther. 2015;16(11):1604-15
LNCaP cells 10 µM 72 h To evaluate the effect of CGI-1746 on prostate cancer cell survival, results showed that CGI-1746 was less effective at killing cells compared to irreversible BTK inhibitors at the same drug concentration. Cancer Biol Ther. 2015;16(11):1604-15

Ibrutinib/伊布替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice HEK293/MRP1 cell xenograft model Oral 30 mg/kg Every other day for 7 days To evaluate the inhibitory effect of PCI 29732 combined with vincristine on the growth of MRP1-overexpressing tumors, results showed that the combination therapy significantly inhibited tumor growth Br J Pharmacol. 2014 Dec;171(24):5845-57.
Mice Pristane-induced plasma cell (PC) tumor model Oral 10 mg/kg Once daily for 70 days Increased the formation of AID-dependent tumors Nature. 2017 Feb 23;542(7642):489-493.
Mice P53ER/ER;LSLKRasG12D;Pdx1-cre mice Drinking water 0.16 mg/mL Daily for 4 weeks Ibrutinib significantly diminished fibrosis, extended survival, and improved the response to clinical standard-of-care therapy. Cancer Res. 2015 Apr 15;75(8):1675-81
Mice EMT6 mammary tumor model Drinking water 25 mg/kg Daily, for two weeks Ibrutinib treatment significantly reduced the frequency of MDSCs in both the spleen and tumor, and improved the efficacy of anti-PD-L1 checkpoint blockade. Cancer Res. 2016 Apr 15;76(8):2125-36.
BALB/C nude mice U87 xenograft model Intraperitoneal injection 6 mg/kg Every other day, for 22 days Ibrutinib induced autophagy and exerted antitumor effect in the U87 xenograft model, and the combination of 3MA with Ibrutinib enhanced the antitumor effect. J Exp Clin Cancer Res. 2017 Jul 17;36(1):96.
Wild-type mice Wild-type mice Intraperitoneal injection 10 mg/kg Daily for 3 days Ibrutinib significantly reduced LPS-induced microglial/astrocyte activation and COX-2 and IL-1β proinflammatory cytokine levels. J Neuroinflammation. 2018 Sep 19;15(1):271.

Ibrutinib/伊布替尼 动物研究

Dose Mice[3]: min = 2.5 mg/kg, max = 25 mg/kg
Administration p.o.

Ibrutinib/伊布替尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02824029 Classical Hodgkin Lymphoma ... 展开 >> Recurrent Hodgkin Lymphoma Refractory Hodgkin Lymphoma 收起 << Phase 2 Recruiting February 2019 United States, Michigan ... 展开 >> Wayne State University/Karmanos Cancer Institute Recruiting Detroit, Michigan, United States, 48201 Contact: Radhakrishnan Ramchandren    313-576-8739       Principal Investigator: Radhakrishnan Ramchandren, M.D.          Sub-Investigator: Divaya Bhutani, M.D.          Sub-Investigator: Jay Yang, M.D.          Sub-Investigator: Jeffrey Zonder, M.D.          Sub-Investigator: Charles Schiffer, M.D.          Sub-Investigator: Abhinav Deol, M.D.          United States, Texas M D Anderson Cancer Center Not yet recruiting Houston, Texas, United States, 77030 Contact: Michelle A. Fanale    713-792-2860    mfanale@mdanderson.org    Principal Investigator: Michelle A. Fanale 收起 <<
NCT03021460 Metastatic Melanoma ... 展开 >> Stage III Skin Melanoma Stage IIIA Skin Melanoma Stage IIIB Skin Melanoma Stage IIIC Skin Melanoma Stage IV Skin Melanoma 收起 << Phase 2 Recruiting February 1, 2021 United States, Minnesota ... 展开 >> Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referral Office    855-776-0015       Principal Investigator: Matthew S. Block 收起 <<
NCT02899078 Metastatic Renal Cell Cancer ... 展开 >> Stage IV Renal Cell Cancer 收起 << Phase 1 Phase 2 Recruiting May 2020 United States, California ... 展开 >> University of California Davis Comprehensive Cancer Center Recruiting Sacramento, California, United States, 95817 Contact: Primo N. Lara, M.D.    916-734-3771    pnlara@ucdavis.edu    Principal Investigator: Primo N. Lara, M.D.          Sub-Investigator: Chong-Xian Pan, M.D., Ph.D. 收起 <<

Ibrutinib/伊布替尼 参考文献

[1]Honigberg LA, Smith AM, 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]Pan Z, Scheerens H, et al. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem. 2007 Jan;2(1):58-61.

Ibrutinib/伊布替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.14mL

22.70mL

4.54mL

2.27mL

Ibrutinib/伊布替尼 技术信息

CAS号936563-96-1
分子式C25H24N6O2
分子量 440.5
SMILES Code C=CC(N1CCC[C@@H](N2C3=C(C(N)=NC=N3)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=N2)C1)=O
MDL No. MFCD20261150
别名 依鲁替尼 ;PCI-32765; Imbruvica; PCI32765, PCI-32765, PCI 32765, Ibrutinib, Imbruvica
运输蓝冰
InChI Key XYFPWWZEPKGCCK-GOSISDBHSA-N
Pubchem ID 24821094
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 105 mg/mL(238.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Ibrutinib | PCI-32765;Imbruvica;PCI32765, PCI-32765, PCI 32765, Ibrutinib, Imbruvica | 依鲁替尼 | BTK | AmBeed-信号通路专用抑制剂 | Ibrutinib/伊布替尼 纯度/质量文件 | Ibrutinib/伊布替尼 亚型比较 | Ibrutinib/伊布替尼 生物活性 | Ibrutinib/伊布替尼 动物研究 | Ibrutinib/伊布替尼 临床数据 | Ibrutinib/伊布替尼 参考文献 | Ibrutinib/伊布替尼 实验方案 | Ibrutinib/伊布替尼 技术信息

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