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PCI 29732 {[allProObj[0].p_purity_real_show]}

货号:A447708 Ambeed 开学季,买赠积分,赢豪礼

PCI 29732 是一种高效、口服可利用且可逆的 BTK 抑制剂,显示出对 BTK 的 Kiapp 值为 8.2 nM,对 Lck 为 4.6 nM,对 Lyn 为 2.5 nM。

PCI 29732 化学结构 CAS号:330786-25-9
PCI 29732 化学结构
CAS号:330786-25-9
PCI 29732 3D分子结构
CAS号:330786-25-9
PCI 29732 化学结构 CAS号:330786-25-9
PCI 29732 3D分子结构 CAS号:330786-25-9
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PCI 29732 纯度/质量文件 产品仅供科研

货号:A447708 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 BTK 其他靶点 纯度
CGI-1746 +++

BTK, IC50: 1.9 nM

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Spebrutinib ++++

BTK, IC50: <0.5 nM

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Acalabrutinib ++

BTK, IC50: 3nM

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CNX-774 +++

BTK, IC50: <1 nM

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Ibrutinib ++++

BTK, IC50: 0.5 nM

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ONO-4059 analog +

BTK, IC50: 23.9 nM

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RN486 ++

BTK, IC50: 4 nM

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(Z)-LFM-A13 +

BTK, Ki: 1.4 μM

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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。

PCI 29732 生物活性

描述 PCI 29732 serves as a highly effective, orally bioavailable, and reversible inhibitor of BTK, displaying Kiapp values of 8.2 nM for BTK, 4.6 nM for Lck, and 2.5 nM for Lyn. Its inhibitory effect on Itk, another member of the Tec family kinases, is relatively modest. Moreover, PCI 29732 disrupts the activity of ABCG2 by competitively attaching to its ATP-binding site[1].[2].
体内研究

Additionally, by competitively binding to the ATP-binding site of ABCG2, PCI 29732 not only inhibits ABCG2's function but also boosts the anti-tumor effects of chemotherapeutic agents that are substrates of ABCG2[2].

When administered at a dose of 20 mg/kg orally every three days for a total of five times, PCI 29732 significantly augments the anti-cancer performance of Topotecan in a H460/MX20 cell xenograft model in nude mice[2].

体外研究

PCI 29732 demonstrates cytotoxic properties across a variety of cell lines, with IC50 values reported as 7.94 μM for S1 cells, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells[2].

PCI-29732 effectively prevents the transcriptional activation of various B-cell activation genes in human CD20+ B cells following stimulation through the B-cell antigen receptor (BCR)[3].

PCI 29732 参考文献

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

[2]Ge C, et al. PCI29732, a Bruton's Tyrosine Kinase Inhibitor, Enhanced the Efficacy of Conventional Chemotherapeutic Agents in ABCG2-Overexpressing Cancer Cells. Cell Physiol Biochem. 2018;48(6):2302-2317.

[3]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;107(29):13075-13080.

PCI 29732 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

PCI 29732 技术信息

CAS号330786-25-9
分子式C22H21N5O
分子量 371.435
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(134.61 mM),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

无水乙醇: 8 mg/mL(21.54 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

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