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PRIMA-1Met
产品别名
5291-32-7
PRIMA-1Met
APR-246
2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one
基本信息
| Empirical Formula【经验(实验)分子式】 | C10H17NO3 |
| Molecular weight | 199.25 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | 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. 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. |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
安全信息
| Pictograms【象形图】 | GHS07 |
| Signal word【警示用语：】 | Warning |
| Hazard Statements | H315 - H319 |
| Precautionary Statements | P305 + P351 + P338 |
| Hazard Classifications【危险分类】 | Eye Irrit. 2 - Skin Irrit. 2 |
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
