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Merck
모든 사진(1)

Key Documents

SML1789

Sigma-Aldrich

PRIMA-1Met

≥98% (HPLC)

동의어(들):

2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one, APR-246

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About This Item

실험식(Hill 표기법):
C10H17NO3
CAS Number:
Molecular Weight:
199.25
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

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

생화학적/생리학적 작용

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

APR-246/PRIMA-1 MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase
Peng X, et al.
Cell Death & Disease, 4(10), e881-e881 (2013)
Christophe Deben et al.
Cancer letters, 375(2), 313-322 (2016-03-16)
APR-246 (PRIMA-1(Met)) is able to bind mutant p53 and restore its normal conformation and function. The compound has also been shown to increase intracellular ROS levels. Importantly, the poly-[ADP-ribose] polymerase-1 (PARP-1) enzyme plays an important role in the repair of
The mutant p53-targeting compound APR-246 induces ROS-modulating genes in breast cancer cells
Synnott N, et al.
Translational Oncology, 11(6) (2018)
Nobuhisa Yoshikawa et al.
Oncology reports, 35(5), 2543-2552 (2016-03-18)
There is an intensive need for the development of novel drugs for the treatment of epithelial ovarian cancer (EOC), the most lethal gynecologic malignancy due to the high recurrence rate. TP53 mutation is a common event in EOC, particularly in
Vladimir J N Bykov et al.
Frontiers in oncology, 6, 21-21 (2016-02-13)
TP53 is the most frequently mutated gene in cancer. The p53 protein activates transcription of genes that promote cell cycle arrest or apoptosis, or regulate cell metabolism, and other processes. Missense mutations in TP53 abolish specific DNA binding of p53

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