化合物 WYE687|T6732|TargetMol

價(jià)格	￥136	￥197	￥346
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱(chēng):化合物 WYE687	英文名稱(chēng):WYE-687
CAS:1062161-90-3	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 98.98%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T6732

Product Introduction

Bioactivity

名稱(chēng)	WYE-687
描述	WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
細(xì)胞實(shí)驗(yàn)	For cell cycle analysis, cells are seeded in 96-well culture plates at 10,000 cells per well for 24 hours, treated with various inhibitors for 24 hours or 48 hours. Following treatment, cells are harvested, washed with PBS and fixed overnight at -20 °C in 70% ethanol. Cells are washed, stained with propidium iodide and analyzed for cell cycle profile (acquired 5000 cells/well) on Guava PCA-96 instrument according to the Guava Cell Cycle Protocol(Only for Reference)
激酶實(shí)驗(yàn)	DELFIA Format of Purified FLAG-TOR: The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 lM microcystin LR, and 100 lg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1-6 hour) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)- p70S6K antibody (1A5) labeled with Europium-N1- ITC (Eu) (10.4 Eu per antibody). Fortyfive microliters of the terminated kinase reaction mixture are transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hour after which the wells are aspirated and washed once with PBS. One hundred microliters of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). One hundred microliters of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader. Data obtained are used to calculate enzymatic activity and enzyme inhibition by potential inhibitors.
體外活性	免疫復(fù)合物激酶檢測(cè)顯示，WYE-687對(duì)mTORC2特異性底物His6-AKT或mTORC1底物His6-S6K具有劑量依賴性的抑制作用。WYE-687在細(xì)胞模型中劑量依賴性地全面抑制mTOR信號(hào)傳導(dǎo)和AKT功能。WYE-678在MDA361人乳腺癌細(xì)胞中，深度抑制帽依賴型及全局蛋白質(zhì)合成。WYE-687在多種癌細(xì)胞系中顯示出抗增殖效果，包括G1期細(xì)胞周期阻滯和選擇性凋亡。WYE-687在U87 mg、MDA361和LNCap細(xì)胞中下調(diào)血管生成因子VEGF和HIF-1α。[1]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : 60.2 mg/mL (100 mM) DMSO : 60.2 mg/mL (100 mM)
關(guān)鍵字	mTOR \| Mammalian target of Rapamycin \| Phosphoinositide 3-kinase \| WYE 687 \| PI3K \| WYE687 \| inhibit \| WYE-687 \| Inhibitor
相關(guān)產(chǎn)品	(-)-Bornyl acetate \| Quercetin Dihydrate \| Apilimod \| Rapamycin \| SB 202190 \| L-Leucine \| Nintedanib \| Myricetin \| 3-Methyladenine \| Isoprenaline hydrochloride \| Erucic acid \| Bakuchiol
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| 抗卵巢癌化合物庫(kù) \| 抗肥胖化合物庫(kù) \| 抗氧化化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù) \| 酪氨酸激酶分子庫(kù)

關(guān)鍵字： N-[4-[4-(4-嗎啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯|TargetMol

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TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：12年
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