化合物 VE-821|T3032|TargetMol

價格	￥415	￥697	￥1259
包裝	5mg	10mg	25mg

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 VE-821	英文名稱:VE-821
CAS:1232410-49-9	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: 99.97%	產(chǎn)品類別: 抑制劑
貨號: T3032

Product Introduction

Bioactivity

名稱	VE-821
描述	VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays).
細胞實驗	Clonogenic survival assays were performed as described before. Briefly, logarithmically growing cells were plated in triplicate in 6-well tissue culture dishes under oxic (21% O2) or hypoxic conditions (0.5% O2) using an InVivo2 300 chamber. Cells were incubated for 6 h before irradiation under oxia or hypoxia using tightly sealed chambers. The target O2 level was achieved within 6 h of gassing and maintained during irradiation, as confirmed by an OxyLite oxygen probe. Cells irradiated under hypoxia were exposed to normoxia at 1 h post-irradiation. As standard, VE-821 (1 μM) was added 1 h prior to irradiation (6 Gy) and was washed away 72 h after irradiation. For the chemotherapy experiments, cells were initially exposed to increasing concentrations of gemcitabine (5, 10 and 20 nM) for 24 h before addition of the VE-821 (1 μM) for another 72 h. The effect of triple combination of irradiation with VE-821 and gemcitabine was examined as well. Cells were incubated for 10–21 d until colonies were stained with 0.5% crystal violet and counted in a CellCount automated colony counter. Clonogenic survival was calculated and data were fitted in GraphPad Prism 4.0 [2].
激酶實驗	The ability of compounds (e.g., VE-821) to inhibit ATR, ATM or DNAPK kinase activity is tested using a radiometric-phosphate incorporation assay. A stock solution is prepared consisting of the appropriate buffer, kinase, and target peptide. To this is added the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [g-33P]ATP solution and incubated at 25°C. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66 μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose-response data are analyzed using GraphPad Prism software [4].
體外活性	VE-821 在對ATR的選擇性上表現(xiàn)出色，對其相關(guān)的PIKKs，包括ATM、DNA依賴性蛋白激酶（DNA-PK）、哺乳動物雷帕霉素靶蛋白和磷酸肌醇3激酶-γ的交叉反應(yīng)性極小（其Kis分別為16 μM、2.2 μM、>1 μM和3.9 μM）。VE-821在經(jīng)羥基脲處理的HT29癌細胞中阻斷了H2AX的磷酸化，但對用新霉素治療的M059J或HT144細胞線無影響[1]。VE-821顯著提高了PSN-1、MiaPaCa-2和原發(fā)性PancM胰腺癌細胞對放射和吉西他濱的敏感性，無論是在正常氧還是缺氧條件下。VE-821通過ATR抑制顯著阻止了癌細胞中由輻射引起的G2/M階段阻滯[2]。在OVCAR-8細胞中，VE-821（1和4 μM）增強了由拓撲替康和順鉑誘導(dǎo)的Ser139位點上H2AX的磷酸化。VE-821未能阻斷由吉西他濱、拓撲替康或順鉑觸發(fā)的ATR介導(dǎo)的Ser345 Chk1或Ser296自磷酸化[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	DMSO : 69 mg/mL (187.3 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	VE-821 \| ATM and RAD3 related \| VE 821 \| ATM/ATR \| Inhibitor \| Ataxia telangiectasia mutated \| inhibit \| VE821
相關(guān)產(chǎn)品	Schisandrin B \| Ceralasertib \| AZ31 \| Berzosertib \| KU60019 \| Elimusertib \| CP-466722 \| GJ103 sodium salt \| Ro 90-7501 \| NU6027 \| (Z)-Mirin \| Dactolisib
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 \| 激酶抑制劑庫 \| 抗衰老化合物庫 \| 抗肥胖化合物庫 \| DNA 損傷和修復(fù)分子庫 \| 糖酵解化合物庫 \| 表型篩選靶點鑒定庫

關(guān)鍵字： ATR Inhibitor IV|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)和生物學研究的科學家提供優(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，化學事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，從高通量篩選到化學結(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	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學試劑,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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