Maleimide-DOTA

目录号: GC60235纯度: >99.50%同义词: Maleimido-mono-amide-DOTA
马来酰亚胺-DOTA(Maleimide-DOTA)是一种双功能螯合剂,可用于蛋白质的缀合以及放射性金属的标记。

Maleimide-DOTA
Cas No.: 1006711-90-5
规格价格库存数量操作
25mg¥1,782.00现货
1
50mg¥2,700.00现货
1
100mg¥4,212.00现货
1

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产品描述 Description

Maleimide-DOTA is a bifunctional chelating agent that can be used for protein conjugation and labeling of radioactive metals [1]. The maleimide-DOTA molecule consists of a maleimide group that reacts specifically with sulfhydryl (-SH) groups on proteins, peptides, and other molecules to form a stable thioether bond [2]. DOTA (dodecanetetraacetic acid, also known as tetraoxycyclohexane) is a chelating agent that is particularly suitable for lanthanide ions and is also suitable for the chelation of radioactive metals such as 68Ga, 111In, and 177Lu. DOTA forms a stable complex with radioactive gold and can be used in the development of radiopharmaceuticals [3, 4]. Maleimide-DOTA can be used to label radiotherapeutic agents or imaging probes and detect labeled tumors by PET, SPECT, and CT methods[5]. The chemical formula of maleimide-DOTA is C22H34N6O9 and the molecular weight is 526.54. This product is for research use only and is not intended for use as food, drug, medical device, or cosmetic.

References:
[1] Nakashima K, Watanabe H, Ono M. Development of Novel Trifunctional Chelating Agents That Enhance Tumor Retention of Radioimmunoconjugates[J]. Journal of Medicinal Chemistry, 2023, 66(18): 12812-12827.
[2] Dijkgraaf I, Agten S M, Bauwens M, et al. Strategies for Site-Specific Radiolabeling of Peptides and Proteins[J]. Radiopharmaceuticals—Current Research for Better Diagnosis and Therapy, 2022.
[3] Wängler C, Schäfer M, Schirrmacher R, et al. DOTA derivatives for site-specific biomolecule-modification via click chemistry: synthesis and comparison of reaction characteristics[J]. Bioorganic & medicinal chemistry, 2011, 19(12): 3864-3874.
[4] Orlova A, Jonsson A, Rosik D, et al. Site-specific radiometal labeling and improved biodistribution using ABY-027, a novel HER2-targeting Affibody molecule–albumin-binding domain fusion protein[J]. Journal of Nuclear Medicine, 2013, 54(6): 961-968.
[5] Wållberg H, Ståhl S. Design and evaluation of radiolabeled tracers for tumor imaging[J]. Biotechnology and applied biochemistry, 2013, 60(4): 365-383.

马来酰亚胺-DOTA(Maleimide-DOTA)是一种双功能螯合剂,可用于蛋白质的缀合以及放射性金属的标记[1]。Maleimide-DOTA分子由马来酰亚胺基团组成,其特异性地与蛋白质、肽和其他分子上的巯基(-SH)反应,形成稳定的硫醚键[2]。DOTA(十二烷四乙酸,也称为四氧环己烷)是一种络合剂,特别适用于镧系离子,也适用于放射性金属如68Ga、111In和177Lu的螯合,DOTA与放射性金形成稳定的复合物可用于放射性药物的开发[3, 4]。Maleimide-DOTA可用于标记放射治疗剂或成像探针,并通过PET、SPECT和CT方法检测标记的肿瘤[5]。Maleimide-DOTA的化学式为C22H34N6O9,分子量为526.54。本产品仅供研究用途,不适用于食品、药品、医疗器械或化妆品。

实验参考方法 Experimental Reference Method

本方案仅提供一个指导,请根据您的具体需要进行修改。

1. 溶液配制
(1)工作液:称量固体,用实验缓冲液稀释到所需的工作浓度。
注意:固体避光保存在-20°C或-80°C。最佳的工作浓度请根据实际情况调整或参阅文献自行设置梯度浓度进行摸索。工作液必须现配现用。


2.采用Maleimide-DOTA用于蛋白质标记的实验步骤[1](来自文献,仅做参考)
(1)二硫键还原蛋白:将蛋白质溶解于PBS(pH 7.4)中。添加280倍摩尔过量的DTT,使最终DTT浓度达到20 mM。将混合物在40°C下孵育30min。
(2)还原蛋白的纯化:使用NAP-5柱纯化反应混合物以去除 DTT,纯化柱要用脱气的0.2 M NH4OAc(pH 6.5)预平衡。收集含有蛋白质的级分。
(3)与Maleimide-DOTA结合:向纯化的蛋白质中添加11倍摩尔过量的Maleimide-DOTA(溶于0.2 M NH4OAc,pH 6.5)。将混合物在40°C下孵育1h。
(4)结合蛋白的纯化:使用NAP-5柱纯化反应混合物,以去除未结合的Maleimide-DOTA。
(5)蛋白质浓度测量:使用DS-11分光光度计测量蛋白质浓度。
(6)储存:将结合蛋白储存在 0.2 M NH4OAc(pH 6.5)中,温度为−20°C。

注意:本实验提供了一项采用Maleimide-DOTA用于蛋白质标记的参考方案,反应浓度和反应时间可根据实际条件优化。操作应在无菌环境中进行,防止污染物干扰反应。避免直接接触反应试剂。

References:

[1] Deyev S M, Xu T, Liu Y, et al. Influence of the position and composition of radiometals and radioiodine labels on imaging of Epcam expression in prostate cancer model using the DARPin Ec1[J]. Cancers, 2021, 13(14): 3589.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1006711-90-5
同义词
Maleimido-mono-amide-DOTA
SMILES
O=C(O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(NCCN2C(C=CC2=O)=O)=O)CC1
分子式
C22H34N6O9
分子量
526.54 g/mol
溶解性
H<sub>2</sub>O : 100 mg/mL (189.92 mM; Need ultrasonic); DMSO : 100 mg/mL (189.92 mM; ultrasonic and warming and heat to 60°C)
保存条件
-20&#176;C, protect from light
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°C,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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol