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。

TAS-117

CAS No. : 1402602-94-1

MCE 站：TAS-117

产品活性：TAS-117 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 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 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：MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Angiotensin II human  |  Acetylcysteine  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  5-Fluorouracil  |  Sorafenib  |  2-Deoxy-D-glucose  |  SP600125  |  Trametinib  |  Gemcitabine  |  Temozolomide  |  MK-2206 dihydrochloride  |  Decitabine  |  Verteporfin  |  Actinomycin D  |  Etoposide  |  Pexidartinib  |  BAY 11-7082  |  DAPT  |  CCCP  |  Ruxolitinib  |  Rote

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。