索曲妥林|T6278|TargetMol

价格	￥442	￥955	￥1680
包装	1mg	5mg	10mg

最小起订量	1mg
发货地	上海
更新日期	2024-09-29

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产品详情

中文名称:索曲妥林	英文名称:Sotrastaurin
CAS:425637-18-9	品牌: TargetMol
产地: 美国	保存条件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
纯度规格: 99.43%	产品类别: 抑制剂
货号: T6278

Product Introduction

Bioactivity

名称	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).
细胞实验	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].
激酶实验	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].
动物实验	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].
体外活性	在无细胞激酶测定中，Sotrastaurin (AEB071) 抑制了PKC，其K(i)值在亚纳摩尔至低纳摩尔范围内。当T细胞受到刺激时，AEB071显著抑制了原位PKC的催化活性。在原代人类及小鼠T细胞中，低纳摩尔浓度的AEB071处理有效阻断了早期T细胞激活标志[1]。在GNAQ/GNA11突变细胞中，与野生型细胞相比，AEB071观察到生长抑制作用。在GNAQ突变细胞中，AEB071降低了myristoylated alanine-rich C-kinase substrate（PKC的一个底物）、ERK1/2和核糖体S6的磷酸化，但AKT激活仍然持续存在[2]。
体内活性	每日口服Sotrastaurin（80 mg/kg，tid）的处理相较于对照组（vehicle-treated animals）显示出了统计学意义上的肿瘤生长抑制效果，相应地，与对照组相比，治疗组的肿瘤体积变化率为17% [2]。与单独使用AEB071或BYL719相比，联合疗法在肿瘤体积减少方面显著更有效。与对照组（vehicle control）相比，这种效果甚至更加显著 [3]。
存储条件	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)
关键字	inhibit \| Sotrastaurin \| Inhibitor \| Protein kinase C \| AEB-071 \| AEB 071 \| PKC
相关产品	Darovasertib \| α-Vitamin E
相关库	抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗衰老化合物库 \| TGF-β/Smad靶点化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库

关键字：索曲妥林|||AEB071|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （12年）	注册资本	566.265100万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

TargetMol中国（陶术生物）

VIP 3年

公司成立：12年
注册资本：566.265100万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：小分子抑制剂、药物筛选化合物库、药物筛选等
公司地址：静安区江场三路238号8楼

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索曲妥林|T6278|TargetMol相关厂家报价

产品名称	价格		公司名称	报价日期
Sotrastaurin (AEB071)	询价	VIP11年	南京百鑫德诺生物科技有限公司	2024-09-26
aladdin 阿拉丁 S408260 Sotrastaurin (AEB071) 425637-18-9 10mM in DMSO	￥1189.90	VIP1年	上海阿拉丁生化科技股份有限公司	2024-08-16
aladdin 阿拉丁 S125985 Sotrastaurin,泛PKC抑制剂 425637-18-9 98%	￥823.90	VIP12年	上海阿拉丁生化科技股份有限公司	2024-08-16

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