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Merck
CN

528100

PI-103

≥97% (HPLC), PI3-K inhibitor, solid

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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关于此项目

经验公式（希尔记法）:
C19H16N4O3
化学文摘社编号:
371935-74-9
分子量:
348.36
MDL编号:
MFCD11983145
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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产品名称

PI-103, A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

质量水平

100

方案

≥97% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

white

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

N5(CCOCC5)c1nc(nc3c1[o]c4ncccc43)c2cc(ccc2)O

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 key

TUVCWJQQGGETHL-UHFFFAOYSA-N

相关类别

一般描述

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

包装

用惰性气体包装

制备说明

完全溶解可能需要轻微加热。

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

毒性：标准处理（A）

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

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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
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
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
PtdIns(3,4)P2, Lamellipodin, and VASP coordinate actin dynamics during phagocytosis in macrophages.
Monta??o-Rend??n, et al.
The Journal of cell biology, 221 (2023)
Franz F Dressler et al.
Nature communications, 15(1), 4513-4513 (2024-05-28)
Urothelial bladder cancer (UC) has a wide tumor biological spectrum with challenging prognostic stratification and relevant therapy-associated morbidity. Most molecular classifications relate only indirectly to the therapeutically relevant protein level. We improve the pre-analytics of clinical samples for proteome analyses
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相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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