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Merck
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528100

Sigma-Aldrich

PI-103

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

别名:

PI-103, 3-（4-（4-吗啉基）吡啶并[3ʹ，2ʹ：4，5]呋喃并[3，2-d]嘧啶-2-基）苯酚，mTOR抑制剂V，PI 3-K抑制剂V

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About This Item

经验公式（希尔记法）:
C19H16N4O3
CAS号:
371935-74-9
分子量:
348.36
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

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
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

分析证书(COA)

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Florence I Raynaud et al.
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
Qi-Wen Fan et al.
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
Zachary A Knight et al.
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
Evelina Valionyte et al.
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

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