索曲妥林|T6278|TargetMol

價(jià)格	￥442	￥955	￥1680
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:索曲妥林	英文名稱:Sotrastaurin
CAS:425637-18-9	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: 99.43%	產(chǎn)品類別: 抑制劑
貨號(hào): T6278

Product Introduction

Bioactivity

名稱	Sotrastaurin
描述	Sotrastaurin (AEB071) is a potent pan-PKC inhibitor (Kis: 0.95/0.64/2.1/3.2/1.8/0.22 nM for PKCα/βI/δ/ε/η/θ).
細(xì)胞實(shí)驗(yàn)	Jurkat cells (5×10^6 cells) were pretreated for 4 h with 500 nM AEB071 and loaded for 30 min at 37°C in the dark with 5 μM fura-2 acetoxymethyl ester. Dye excess was removed by washing in Hanks' balanced salt solution. Samples were prewarmed to 37°C and baseline Ca2+ levels were determined for 100 s on a Spex Fluorolog 2 spectrofluorometer equipped with two excitation monochrometers and a Cooper system. At this point, anti-CD3 antibody was added to a final concentration of 10 μg/ml, and data were collected over 6.5 min. The maximal and minimal Ca2 levels were determined by adding an excess of ionomycin and EGTA. Experiments were performed at least four times with similar outcomes [1].
激酶實(shí)驗(yàn)	Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in 20 mM Tris-HCl buffer, pH 7.4, and 0.1% bovine serum albumin by incubating 1.5 μM of the peptide substrate with 10 μM [33P]ATP, 10 mM Mg(NO3)2, 0.2 mM CaCl2, and PKC at a protein concentration varying from 25 to 400 ng/ml, and lipid vesicles containing 30 mol% phosphatidylserine, 5 mol% diacylglycerol (DAG), and 65 mol% phosphatidylcholine at a final lipid concentration of 0.5 μM. Incubation was performed for 60 min at room temperature. The reaction was stopped by adding 50 μl of a mixture containing 100 mM EDTA, 200 μM ATP, 0.1% Triton X-100, and 0.375 μg/well streptavidin-coated scintillation proximity assay beads in PBS without Ca2+ and Mg2+. Incorporated radioactivity was measured in a MicroBetaTrilux counter for 1 min. In situ Thr-219 autophosphorylation status analysis of PKC was done by a phospho-site-specific antibody [1].
動(dòng)物實(shí)驗(yàn)	6–8 week nu/nu SCID female mice bearing subcutaneously injected 92.1 tumors (7 mice/group) of 100mm3 diameter were treated with vehicle, AEB071 (80mg/kg/d) TID and or BYL719 orally (50mg/kg/d) QD as single agents and in combination, 5 days/week for 2 weeks. After 2 weeks, two animals from each group were sacrificed and tumors were collected to analyze for Western blot. For Omm1 xenografts, 6–8 weeks athymic female mice bearing subcutaneously injected Omm1 tumors (7 mice/group) of 100 mm3 diameter were treated with vehicle, AEB071 (80mg/kg/d) TID and or BYL719 orally (50mg/kg/d) QD as single agents and in combination, 5 days/week for 3 weeks. Tumors were homogenized with grinding resins kits as per manufacturer's instructions. Tumors were collected to analyze for H&E and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) staining. Tumors were measured every 2 to 3 days with calipers, and tumor volumes were calculated by the formula 4/3 × r3 [r = (larger diameter + smaller diameter)/4. Toxicity was monitored by weight loss [3].
體外活性	在無細(xì)胞激酶測(cè)定中，Sotrastaurin (AEB071) 抑制了PKC，其K(i)值在亞納摩爾至低納摩爾范圍內(nèi)。當(dāng)T細(xì)胞受到刺激時(shí)，AEB071顯著抑制了原位PKC的催化活性。在原代人類及小鼠T細(xì)胞中，低納摩爾濃度的AEB071處理有效阻斷了早期T細(xì)胞激活標(biāo)志[1]。在GNAQ/GNA11突變細(xì)胞中，與野生型細(xì)胞相比，AEB071觀察到生長抑制作用。在GNAQ突變細(xì)胞中，AEB071降低了myristoylated alanine-rich C-kinase substrate（PKC的一個(gè)底物）、ERK1/2和核糖體S6的磷酸化，但AKT激活仍然持續(xù)存在[2]。
體內(nèi)活性	每日口服Sotrastaurin（80 mg/kg，tid）的處理相較于對(duì)照組（vehicle-treated animals）顯示出了統(tǒng)計(jì)學(xué)意義上的腫瘤生長抑制效果，相應(yīng)地，與對(duì)照組相比，治療組的腫瘤體積變化率為17% [2]。與單獨(dú)使用AEB071或BYL719相比，聯(lián)合療法在腫瘤體積減少方面顯著更有效。與對(duì)照組（vehicle control）相比，這種效果甚至更加顯著 [3]。
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	DMSO : 81 mg/mL (184.7 mM) Ethanol : 2 mg/mL (4.56 mM)
關(guān)鍵字	inhibit \| Sotrastaurin \| Inhibitor \| Protein kinase C \| AEB-071 \| AEB 071 \| PKC
相關(guān)產(chǎn)品	Darovasertib \| α-Vitamin E
相關(guān)庫	抗癌活性化合物庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 抗衰老化合物庫 \| TGF-β/Smad靶點(diǎn)化合物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫

關(guān)鍵字：索曲妥林|||AEB071|TargetMol

公司簡(jiǎn)介

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)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫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，以及多種類型的生化試劑產(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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