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化合物 PI103,PI-103

化合物 PI103|T6143|TargetMol

價(jià)格 353 822 1280
包裝 1mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-02
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產(chǎn)品詳情

中文名稱:化合物 PI103英文名稱:PI-103
CAS:371935-74-9品牌: TargetMol
產(chǎn)地: 美國保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格: 99.3%產(chǎn)品類別: 抑制劑
貨號: T6143
2024-12-02 化合物 PI103 PI-103 1mg/353RMB;5mg/822RMB;10mg/1280RMB 353 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.3% 抑制劑

Product Introduction

Bioactivity

名稱PI-103
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).
細(xì)胞實(shí)驗(yàn)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].
激酶實(shí)驗(yàn)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].
動物實(shí)驗(yàn)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].
體外活性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].
體內(nèi)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].
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 5 mg/mL (14.35 mM), Sonication is recommended.
關(guān)鍵字PI3K | Phosphoinositide 3-kinase | Inhibitor | DNA-PK | Apoptosis | Autophagy | DNA-dependent protein kinase | inhibit | Mammalian target of Rapamycin | PI-103 | mTOR
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相關(guān)庫抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 氧化還原化合物庫 | 自噬庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 抗肺癌化合物庫 | 酪氨酸激酶分子庫
關(guān)鍵字: PI103|||PI 103|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部,化學(xué)事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實(shí)體化合物分子供應(yīng);從商業(yè)化產(chǎn)品銷售到個性化定制合成;從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選,從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化,我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。 經(jīng)過在中國市場五年的精心耕耘,我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商,為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期 2013-04-18 (12年) 注冊資本 566.2651萬人民幣
員工人數(shù) 100-500人 年?duì)I業(yè)額 ¥ 1億以上
主營行業(yè) 化學(xué)試劑,生物活性小分子 經(jīng)營模式 貿(mào)易,試劑,定制,服務(wù)
  • TargetMol中國(陶術(shù)生物)
VIP 12年
  • 公司成立:12年
  • 注冊資本:566.2651萬人民幣
  • 企業(yè)類型:有限責(zé)任公司(自然人投資或控股)
  • 主營產(chǎn)品:小分子抑制劑,藥物篩選化合物庫,天然產(chǎn)物,活性分子化合物等
  • 公司地址:上海市閘北區(qū)江場三路28號4樓
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