PCI-32765 (Ibrutinib)
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PCI-32765 (Ibrutinib)是Bruton tyrosine kinase(BTK)的抑制剂,被用于研究BTK对成熟B细胞功能和B细胞相关疾病发展的生物学效应。BTK是BCR信号所必须的。人和小鼠中扰乱BTK功能的突变可以阻止B细胞的成熟,而B细胞的成熟需要功能性BCR途径的参与。PCI-32765还可以抑制自身抗体的产生。在体外和体内试验中,通过使用BTK亲和性的荧光探针检测到PCI-32765占据了BTK的活性位点。
参考文献:
1. Lee A. Honigberga, Ashley M. Smitha, Mint Sirisawada, Erik Vernera, David Lourya, Betty Changa, Shyr Lib, Zhengying Panb,d, Douglas H. Thamme, Richard A. Millera, and Joseph J. Buggya. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. PNAS. 2010; 107(29): 13075 – 80.
- 1. Suyog Pol, Ravendra Dhanraj, et al. "Protective Effect of Bruton Tyrosine Kinase Inhibitor in Murine Model of Chronic Demyelination." Research Square September 27th, 2022.
- 2. Madison Barbara Allerton Hagger. "The Synergy of Adenosine and Ibrutinib on Platelet Aggregation in Chronic Lymphocytic Leukemia." Murdoch University 2021.
- 3. Alhakeem SS, McKenna MK, et al. "Chronic Lymphocytic Leukemia-Derived IL-10 Suppresses Antitumor Immunity." J Immunol. 2018 Jun 15;200(12):4180-4189. PMID: 29712773
- 4. Schroeder JT, Bieneman AP. "Activation of Human Basophils by A549 Lung Epithelial Cells Reveals a Novel IgE-Dependent Response Independent of Allergen." J Immunol. 2017 Aug 1;199(3):855-865. PMID: 28652400
- 5. Kosowicz JG, Lee J, et al. "Drug modulators of B cell signaling pathways and Epstein-Barr virus lytic activation." J Virol. 2017 May 31. pii: JVI.00747-17. PMID: 28566383
- 6. Lee DD, Muskaj I, et al. "Platelet proteins cause basophil histamine release through an immunoglobulin-dependent mechanism." Transfusion. 2017 May 4. PMID: 28470742
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 440.5 |
Cas No. | 936563-96-1 |
Formula | C25H24N6O2 |
Synonyms | PCI-32765, Ibrutinib, CRA-032765 |
Solubility | ≥22.02 mg/mL in DMSO; insoluble in H2O; ≥10.4 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide |
SDF | Download SDF |
Canonical SMILES | C=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验: | |
细胞系 |
CLL细胞系 |
溶解方法 |
在DMSO中的溶解度 >10 mM。为了获得更高的浓度,可以将离心管在37°C 加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20°C 以下储存几个月。 |
反应条件 |
1 μM;24 h、48 h和72 h |
应用 |
在CLL细胞中,PCI-32765处理24 h、48 h和72 h后均减少anti-IgM支持的细胞活力,从69%分别减少到33%、31%和29%。与非刺激对照相比,anti-IgM刺激24 h后诱导细胞活力平均增加27%±12%。而与非刺激对照相比,在anti-IgM刺激之前,用1 μM PCI-32765处理显著减少CLL细胞的活力到98%±8%。PCI-32765也可以有效抑制来自NLCs的存活信号。 |
动物实验: | |
动物模型 |
CB17 SCID小鼠和Eμ-TCL1转基因(Tg)C3H/BL6小鼠 |
剂量 |
次优(2.5 mg/kg/d);最佳(25 mg/kg/d) |
应用 |
在过继转移TCL1小鼠模型中,细胞转移两周后分别用次优(2.5 mg/kg/d)和最佳(25 mg/kg/d)剂量的PCI-32765处理,小鼠在第4天出现瞬态淋巴细胞增多,并分别增加了7倍和10倍的循环TCL1白血病细胞。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Ponader S, Chen S S, Buggy J J, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo[J]. Blood, 2012, 119(5): 1182-1189. |
描述 | Ibrutinib是一种有效的、高选择性的Bruton's tyrosine kinase (BTK)抑制剂,IC50值为0.5 nM,对Bmx、CSK、 FGR、 BRK及HCK中度有效,对EGFR、Yes、ErbB2、JAK3等作用效果较弱。 | |||||
靶点 | Btk | |||||
IC50 | 0.5 nM |
质量控制和MSDS
- 批次:
化学结构
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