推薦產品
品質等級
化驗
≥97% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
white
溶解度
DMSO: 5 mg/mL
運輸包裝
ambient
儲存溫度
−20°C
InChI
1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2
InChI 密鑰
TUVCWJQQGGETHL-UHFFFAOYSA-N
一般說明
一种可渗透细胞的吡啶基呋喃嘧啶化合物,可作为DNA-PK,PI3-K和mTOR的强效和ATP竞争性抑制剂(DNA-PK,p110α,p110β,p110δ,p110γ,PI3-KC2β,mTORC1和mTORC2的IC50分别为2、8、88、48、150、26、20和83 nM)。 它仅在更高的浓度(分别为IC50=850和920 nM)下抑制ATR和ATM,并且即使在浓度高为10 µM时,对一组40多种其他激酶也几乎没有活性。已证明可有效阻断体外和体内胶质瘤细胞系中的PI3-K/Akt信号传导和细胞增殖。也可购买10 mM(2 mg/574 µl)PI-103 DMSO溶液(目录号528101)。
生化/生理作用
主要靶标
DNA-PK,PI3-K和mTOR
DNA-PK,PI3-K和mTOR
产物与ATP竞争。
可逆:否
细胞可渗透性:具有
靶标IC50:DNA-PK,p110α,p110β,p110delta;,p110γ,PI3-KC2β,mTORC1和mTORC2分别为2、8、88、48、150、26、20和83 nM
包裝
用惰性气体包装
警告
毒性:标准处理(A)
準備報告
完全溶解可能需要轻微加热。
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號,寫有 ‘Lot’或‘Batch’.。
Cancer research, 67(12), 5840-5850 (2007-06-19)
Extensive evidence implicates activation of the lipid phosphatidylinositide 3-kinase (PI3K) pathway in the genesis and progression of various human cancers. PI3K inhibitors thus have considerable potential as molecular cancer therapeutics. Here, we detail the pharmacologic properties of a prototype of
Cancer cell, 9(5), 341-349 (2006-05-16)
The PI3 kinase family of lipid kinases promotes cell growth and survival by generating the second messenger phosphatidylinositol-3,4,5-trisphosphate. To define targets critical for cancers driven by activation of PI3 kinase, we screened a panel of potent and structurally diverse drug-like
Cell, 125(4), 733-747 (2006-05-02)
Phosphoinositide 3-kinases (PI3-Ks) are an important emerging class of drug targets, but the unique roles of PI3-K isoforms remain poorly defined. We describe here an approach to pharmacologically interrogate the PI3-K family. A chemically diverse panel of PI3-K inhibitors was
Cell death and differentiation (2021-12-05)
SQSTM1/p62, as a major autophagy receptor, forms droplets that are critical for cargo recognition, nucleation, and clearance. p62 droplets also function as liquid assembly platforms to allow the formation of autophagosomes at their surfaces. It is unknown how p62-droplet formation
文章
AldeRed™ 588-A is a red fluorescent live cell probe that detects ALDH activity used to identify cancer stem cells and progenitor cells in culture.
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