产品名称

英文名称：APR-246

同义词

APR-246、5291-32-7、PRIMA-1MET、Eprenetapopt、2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one、2-(Hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one、APR 246、Eprenetapopt [USAN]、Z41TGB4080、3-Quinuclidinone, 2-(hydroxymethyl)-2-(methoxymethyl)-

产品性质

CAS编号：5291-32-7

分子式：C10H17NO3

分子量：199.25

PubChem编号：52918385

英文别名：APR-246|5291-32-7|PRIMA-1MET|Eprenetapopt|2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one|2-(Hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one|APR 246|Eprenetapopt [USAN]|Z41TGB4080|3-Quinuclidinone, 2-(hydroxymethyl)-2-(methoxymethyl)-

规格或纯度：97%

英文名称：APR-246

生化机理：PRIMA-1Met (APR-246) is a re-activator of mutant p53 activity. It′s the methylated, more potent derivative of PRIMA-1. PRIMA-1Met covalently modifies the core domain of mutated p53 restoring the wild-type conformation and activty of p53 in tumor cells, leading to cell cycle arrest and apoptosis. PRIMA-1Met has also been shown to increase intracellular levels of reactive oxygen species (ROS), which may contribute to its anti-tumor activity. PRIMA-1Met, also called APR-246, is converted to methylene quinuclidinone (MQ), a Michael acceptor. It interacts with p53 through the cysteine (Cys) residue. It blocks the thioredoxin reductase (TrxR1) enzyme. It is under clinical investigation and well-studied. PRIMA-1Met effect is tested on breast cancer specific gene expression.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1(TrxR1), akey regulator of cellular redox balance.PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1(TrxR1), akey regulator of cellular redox balance.

ALogP：-0.1

IUPAC Name：2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one

INCHI：InChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3

InChi Key：BGBNULCRKBVAKL-UHFFFAOYSA-N

Canonical SMILES：COCC1(C(=O)C2CCN1CC2)CO

Isomeric SMILES：COCC1(C(=O)C2CCN1CC2)CO

PubChem CID：52918385

溶解性：DMSO 100 mg/mL (501.88 mM; Need ultrasonic) H2O 50 mg/mL (250.94 mM; Need ultrasonic)

象形图：

信号词：Warning

危险声明：H315 Causes skin irritationH319 Causes serious eye irritation

预防措施声明：P305+P351+P338

产品包装