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Bortezomib (PS-341)

Catalog No.
A2614
蛋白酶体抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 600.00
现货
25mg
¥ 1,080.00
现货
100mg
¥ 2,500.00
现货
500mg
¥ 6,800.00
现货

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Background

Bortezomib (originally codenamed PS-341) is the first therapeutic proteasome inhibitor to the tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. [1] The drug is an N-protected dipeptide and can be written as Pyz-Phe-boroLeu, which stands for pyrazinoic acid, phenylalanine and Leucine with a boronic acid instead of a carboxylic acid. Peptides are written N-terminus to C-terminus, and this convention is used here even though the "C-terminus" is a boronic acid instead of a carboxylic acid. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon suppression of pro-apoptotic pathways. Recently, it was found that bortezomib caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. [2] Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

A potent (Ki = 0.6 nM), specific and reversible proteasome inhibitor. It inhibits cell proliferation of H460 cells (Human non-small cell lung cancer cell lines) with an IC₅₀ of 0.1 µM.

References:
1. Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
2. Gelman JS, Sironi J, Berezniuk I, Dasgupta S, Castro LM, Gozzo FC, Ferro ES, Fricker LD (2013). "Alterations of the intracellular peptidome in response to the proteasome inhibitor bortezomib". In Gartel, Andrei L. PLoS One 8 (8): e53263.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt384.24
Cas No.179324-69-7
FormulaC19H25BN4O4
SynonymsBortezomib,PS-341,LDP-341,MLM341,MG-341,NSC-681239
Solubility≥19.212mg/mL in DMSO
Chemical Name[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
SDFDownload SDF
Canonical SMILESB(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验[1]:

细胞系

犬恶性黑色素瘤细胞系(CMM-1、CMM-2、ChMC、KMeC、LMeC、OMJ、OMS、OMK和NML)

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℃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℃以下储存几个月。

反应条件

72 h;IC50=3.5~5.6 nM

应用

Bortezomib有效抑制细胞生长,而其它化合物对细胞生长没有或有很小的影响。在9个犬恶性黑色素瘤细胞系(CMM-1、CMM-2、ChMC、KMeC、LMeC、OMJ、OMS、OMK和NML)中,bortezomib抑制所有细胞系的生长,IC50范围介于3.5~5.6 nM之间。

动物实验[1]:

动物模型

无胸腺裸鼠

剂量

0.8 mg/kg;静脉注射

应用

在异种移植小鼠模型中评估bortezomib对CMM-1细胞的体内生长抑制活性。在第4天的治疗后,bortezomib显著抑制肿瘤生长(P < 0.01,对照vs. Bortezomib)。与对照相比,bortezomib治疗小鼠的肿瘤具有显著降低的有丝分裂指数(P <0.01)。同样的,bortezomib治疗小鼠来源的肿瘤中,Ki67指数也显著下降(P < 0.01)。

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] Ito K, Kobayashi M, Kuroki S, et al. The proteasome inhibitor bortezomib inhibits the growth of canine malignant melanoma cells in vitro and in vivo[J]. The Veterinary Journal, 2013, 198(3): 577-582.

生物活性

描述 Bortezomib (PS-341)是一个有效的20s蛋白酶体抑制剂,Ki值为0.6 nM。
靶点 20S proteasome          
IC50 0.6 nM (Ki)          

质量控制

化学结构

PS341

相关生物数据

PS341

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PS341

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PS341

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PS341

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PS341

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PS341