推荐产品
质量水平
检测方案
≥97% (HPLC)
形式
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
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
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
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
警告
毒性：标准处理（A）
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
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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)
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