规格 | 25 mg |
数量 | 货期:1-2天 |
保存条件 | 4°C, sealed storage, away from moisture |
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
MCE 国际站:TAS-117 hydrochloride
产品活性:TAS-117 hydrochloride 是一种有效、选择性、具有口服活性的别构 Akt 抑制剂 (对 Akt1、2 和 3 的 IC50 分别为 4.8、1.6 和 44 nM)。TAS-117 hydrochloride 激发抗骨髓瘤活性并增强蛋白酶体抑制诱导的致命内质网应激。TAS-117 hydrochloride 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。
研究领域:PI3K/Akt/mTOR | Apoptosis | Autophagy
作用靶点:Akt | Apoptosis | Autophagy
In Vitro: TAS-117 (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt.
TAS-117 (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt.
TAS-117 abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. TAS-117 enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. TAS-117 (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response.
TAS-117 enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that TAS-117 augments Bortezomib-induced ER stress and apoptotic signaling.
In Vivo: TAS-117 (12-16 mg/kg; p.o.; daily for 5 days a week, 21 days) inhibits tumor growth in murine xenograft models of human MM.
TAS-117 enhances bortezomib-induced MM cytotoxicity in vivo.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Endoplasmic Reticulum Stress Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Angiogenesis Related Compound Library | Glucose Metabolism Compound Library | Anti-Liver Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Y-27632 dihydrochloride | Paclitaxel | Acetylcysteine | Angiotensin II human | Tamoxifen | Staurosporine | 5-Fluorouracil | 2-Deoxy-D-glucose | Bortezomib | Sorafenib | SP600125 | Trametinib | Gemcitabine | Temozolomide | Verteporfin | MK-2206 dihydrochloride | Decitabine | Etoposide | CCCP | Rotenone | DAPT | Ruxolitinib | BAY 11-7082 | Actinomycin D | Pexidartinib
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 染料试剂 | PROTAC | 同位素标记物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物;
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。