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  • 索曲妥林|T6278|TargetMol

索曲妥林|T6278|TargetMol

Sotrastaurin
425637-18-9
442 1mg 起订
955 5mg 起订
1680 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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产品详情:

中文名称:
索曲妥林
英文名称:
Sotrastaurin
CAS号:
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
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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 (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
经营模式 贸易,工厂,试剂,定制,服务
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

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