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PI-103

PI-103

产品编号 T6143   CAS 371935-74-9
别名: PI103, PI 103

PI-103 是一种 PI3KmTOR 抑制剂,抑制 p110α、p110β、p110δ、p110γ、mTORC1和 mTORC2,IC50分别为 8 nM、88 nM、48 nM、150 nM、20 nM 和 83 nM。它可诱导自噬,还抑制 DNA-PK,IC50为 2 nM。

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PI-103 Chemical Structure
PI-103, CAS 371935-74-9
规格 价格/CNY 货期 数量
1 mg ¥ 353 现货
5 mg ¥ 822 现货
10 mg ¥ 1,280 现货
25 mg ¥ 1,980 现货
50 mg ¥ 2,880 现货
100 mg ¥ 3,490 现货
200 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 861 现货
其他形式的 PI-103:
产品目录号及名称: PI-103 (T6143)
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纯度: 99.3%
纯度: 97.82%
纯度: 96.59%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).
靶点活性 mTOR:30 nM (cell free), p110α:2 nM (cell free), p110γ:15 nM (cell free), DNA-PK:23 nM (cell free), p110δ:3 nM (cell free), p110β:3 nM (cell free)
体外活性 PI-103 potently inhibited p110α (IC50: 15 nmol/L. PI-103 exhibited potent growth inhibition in each of the cell lines examined, with activity in the submicromolar range [1]. PI-103 induced proliferative arrest in a panel of glioma cell lines assayed by flow cytometry. PI-103 uniquely and potently inhibits both complexes of mTOR: the rapamycin-sensitive mTORC1 (IC50: 0.02 μM) and the rapamycin-insensitive mTORC2 (IC50: 0.083 μM). PI-103 (IC50 < 0.1 μM) was blocking the phosphorylation of p70 S6 kinase, ribosomal protein S6, and 4E-BP1, downstream markers of mTOR signaling [2].
体内活性 When tumors reached 50–100 mm^3, animals were randomized and treated with vehicle or PI-103. PI-103 showed significant activity in vivo, reducing average tumor size by 4-fold after 18 days. Preclinical treatment of glioma xenografts with PI-103 blocked proliferation without inducing apoptosis [2]. PI-103 (10 mg/kg) treatment promoted a significant in vivo tumor growth compared with the DMSO treated mice. PI-103 (70 mg/kg) also promoted a significant in vivo tumor growth [3].
激酶实验 Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software [1].
细胞实验 Human glioma cell lines were obtained from the Brain Tumor Research Center at UCSF. Cells were harvested and fixed, treated with RNAase and propidium iodide, and filtered through 95 mM nylon mesh. Ten thousand stained nuclei were analyzed in a FACS Calibur flow cytometer. DNA histograms were modeled offline using Modifit-LT software. For crystal violet staining, 10^5 cells were seeded in 12-well plates in the presence or absence of PI-103 [2].
动物实验 Five to six-month-old males of either FVB/N strain or nude BALB/c strain were injected subcutaneously with one million cells in PBS. When the tumor reached between 50 and 100 mm^3, mice were treated with the inhibitors. Treatments were done by IP injection daily with 10 mg/kg or 70 mg/kg of PI-103 and/or 50 mg/kg sorafenib. Control mice were treated with the same volume of DMSO. Tumor size and mice weight was monitored every 2 days. Tumor volume was calculated with the equation (d^2*D) (p/6). When mice were sacrificed, tumors were dissected and processed. For immunosuppression experiments, mice were treated with rapamycin (1 mg/kg) or LY294002 (25 mg/kg) by a daily IP injection for a total of 8 days [3].
别名 PI103, PI 103
分子量 348.36
分子式 C19H16N4O3
CAS No. 371935-74-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 23 mg/mL (66 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8706 mL 14.353 mL 28.7059 mL 71.7648 mL
5 mM 0.5741 mL 2.8706 mL 5.7412 mL 14.353 mL
10 mM 0.2871 mL 1.4353 mL 2.8706 mL 7.1765 mL
20 mM 0.1435 mL 0.7176 mL 1.4353 mL 3.5882 mL
50 mM 0.0574 mL 0.2871 mL 0.5741 mL 1.4353 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-38. 2. Fan QW, et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell. 2006 May;9(5):341-9. 3. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of sorafenib-treated melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61.
YH239-EE Cysteamine hydrochloride Sodium salicylate Indirubin Tebufenozide ULK1-IN-2 Liensinine Schinifoline

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌活性化合物库 活性脂质化合物库 DNA 损伤和修复分子库 抗癌化合物库 激酶抑制剂库 抗氧化化合物库 抗乳腺癌化合物库 抗抑郁症化合物库 PI3K/Akt/mTOR 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PI-103 371935-74-9 Apoptosis Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling PI3K DNA-PK mTOR Phosphoinositide 3-kinase Inhibitor PI103 DNA-dependent protein kinase inhibit Mammalian target of Rapamycin PI 103 inhibitor

 

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