おすすめの製品
品質水準
アッセイ
≥98% (HPLC)
形状
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear
保管温度
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
生物化学的／生理学的作用
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.
シグナルワード
Warning
危険有害性情報
危険有害性の分類
Eye Irrit. 2 - Skin Irrit. 2
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML1789-VAR:
SML1789-25MG:
SML1789-5MG:
SML1789-BULK:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
製品に関するお問い合わせはこちら（テクニカルサービス）