Pimonidazole
(Synonyms: 哌莫硝唑) 目录号 : GC41338Pimonidazole是一种缺氧标志物,用于肿瘤内缺氧和细胞增殖的研究。
Cas No.:70132-50-2
Sample solution is provided at 25 µL, 10mM.
Pimonidazole is an anoxic marker used in studying intratumoral hypoxia and cell proliferation. Pimonidazole is a 2-nitroimidazole that is reductively activated specifically in hypoxic cells and forms stable adducts with thiol groups in proteins, peptides, and amino acids. The amount of Pimonidazole that is detected is directly proportional to the level of hypoxia within tumors [1-3].
Pimonidazole (80mg/kg; i.p) can be used to study hypoxia near necrosis of C6 rat brain glioma[4]. Pimonidazole can be used as an investigational hypoxia probe in clinical trials. Patients with primary cervical squamous cell carcinoma received a single infusion of Pimonidazole (0.5g/m²; i.v), followed by tumor biopsies 24 hours later. Immunohistochemical staining confirmed hypoxic cells, aiding tumor hypoxia assessment before radiation therapy[5]. 39 intermediate/high risk prostate cancer patients received a single oral dose of Pimonidazole (0.5g/m2) 24h prior to radical prostatectomy surgery. Pimonidazole-defined hypoxia intensity was positively correlated with advanced pathologic stage, tumor invasion, and cribriform and intraductal carcinoma morphology[6]. Pimonidazole can be used as an exogenous hypoxia marker for matrix-assisted laser desorption/ionization (MALDI) MSI. In hypoxic cells, Pimonidazole is reduced and forms reactive products that bind to thiol groups in proteins, peptides, and amino acids. A reductively activated Pimonidazole metabolite can be imaged by MALDI-MSI in a breast tumor xenograft model[7].
References:
[1]. Varia MA, Calkins-Adams DP, et,al. Pimonidazole: a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in cervical carcinoma. Gynecol Oncol. 1998 Nov;71(2):270-7. doi: 10.1006/gyno.1998.5163. PMID: 9826471.
[2]. Inci ID, Tekin V, et,al. Radioiodination of Pimonidazole as a Novel Theranostic Hypoxia Probe. Curr Radiopharm. 2021;14(1):46-50. doi: 10.2174/1874471013666200331114908. PMID: 32228432.
[3]. Aguilera KY, Brekken RA. Hypoxia Studies with Pimonidazole in vivo. Bio Protoc. 2014 Oct 5;4(19):e1254. doi: 10.21769/bioprotoc.1254. PMID: 27453908; PMCID: PMC4956402.
[4]. Zoula S, Rijken PF, et,al. Pimonidazole binding in C6 rat brain glioma: relation with lipid droplet detection. Br J Cancer. 2003 May 6;88(9):1439-44. doi: 10.1038/sj.bjc.6600837. PMID: 12778075; PMCID: PMC2741029.
[5]. Kennedy AS, Raleigh JA, et,al. Proliferation and hypoxia in human squamous cell carcinoma of the cervix: first report of combined immunohistochemical assays. Int J Radiat Oncol Biol Phys. 1997 Mar 1;37(4):897-905. doi: 10.1016/s0360-3016(96)00539-1. PMID: 9128967.
[6]. Ci X, Chen S, et,al. Oral pimonidazole unveils clinicopathologic and epigenetic features of hypoxic tumour aggressiveness in localized prostate cancer. BMC Cancer. 2024 Jun 18;24(1):744. doi: 10.1186/s12885-024-12505-1. PMID: 38890593; PMCID: PMC11186205.
[7]. Mascini NE, Cheng M, et,al. Mass Spectrometry Imaging of the Hypoxia Marker Pimonidazole in a Breast Tumor Model. Anal Chem. 2016 Mar 15;88(6):3107-14. doi: 10.1021/acs.analchem.5b04032. Epub 2016 Feb 29. PMID: 26891127.
Pimonidazole是一种缺氧标志物,用于肿瘤内缺氧和细胞增殖的研究。Pimonidazol是一种2-硝基咪唑,在缺氧细胞中被特异性还原激活,并与蛋白质、肽和氨基酸中的巯基形成稳定的加合物。Pimonidazole的检出量与肿瘤内缺氧程度成正比[1-3]。
Pimonidazole(80mg/kg; i.p)可用于研究C6大鼠脑胶质瘤坏死附近的缺氧情况[4]。Pimonidazole可用作临床试验中的研究性缺氧探针。患有原发性宫颈鳞状细胞癌的患者接受了单次pimonidazole (0.5g/m²; i.v),24小时后进行肿瘤活检。免疫组化染色证实了缺氧细胞的存在,这有助于在放疗前评估肿瘤缺氧情况[5]。39名中高风险前列腺癌患者在接受根治性前列腺切除术前24小时单次口服Pimonidazole(0.5g/m2)。Pimonidazole定义的缺氧强度与晚期病理分期、肿瘤侵袭以及筛状和导管内癌形态呈正相关[6]。Pimonidazole可用作基质辅助激光解吸电离(MALDI)质谱成像(MSI)的外源性缺氧标志物。在缺氧细胞中,Pimonidazole被还原并形成可与蛋白质、肽和氨基酸中的巯基结合的反应性产物。还原激活的Pimonidazole代谢物可通过MALDI-MSI在乳腺肿瘤异种移植模型中成像[7]。
C6大鼠脑胶质瘤缺氧切片的制备[1]:
1. 脑胶质瘤实验模型:将5μl C6细胞悬液,105个细胞立体定向注射于6只雌性Wistar大鼠右侧尾状核硬脑膜下3mm处(160-180g)。
2. 实验在肿瘤发育结束时(肿瘤细胞植入后22-25天)进行。
3. 大鼠注射0.25mlPimonidazole磷酸盐缓冲盐水(PBS, pH 7.4)溶液(80mg/kg体重)。
4. 这些标记物分别在杀死前60分钟和1分钟通过尾静脉静脉给药。 迅速取脑(大鼠死亡后不超过3min),用液氮冷冻,- 80℃保存。
5. 对每只大鼠在肿瘤中部(肿瘤最大的地方)取5μm厚的横切面,在数字图像分析系统上进行分析。
本实验来自文献,请根据具体情况进行修改
References:
[1]. Zoula S, Rijken PF, et,al. Pimonidazole binding in C6 rat brain glioma: relation with lipid droplet detection. Br J Cancer. 2003 May 6;88(9):1439-44. doi: 10.1038/sj.bjc.6600837. PMID: 12778075; PMCID: PMC2741029.
Cas No. | 70132-50-2 | SDF | |
别名 | 哌莫硝唑 | ||
化学名 | α-[(2-nitro-1H-imidazol-1-yl)methyl]-1-piperidineethanol | ||
Canonical SMILES | OC(CN1CCCCC1)CN2C([N+]([O-])=O)=NC=C2 | ||
分子式 | C11H18N4O3 | 分子量 | 254.3 |
溶解度 | 10mg/mL in ethanol,or DMSO of DMF | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.9324 mL | 19.6618 mL | 39.3236 mL |
5 mM | 0.7865 mL | 3.9324 mL | 7.8647 mL |
10 mM | 0.3932 mL | 1.9662 mL | 3.9324 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet