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。

Alvespimycin

CAS No. : 467214-20-6

MCE 站：Alvespimycin

产品活性：Alvespimycin (17-DMAG) 是一种有效的 Hsp90 抑制剂，结合到 Hsp90，EC₅₀ 为 62 ± 29 nM。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease

作用靶点：HSP

In Vitro: Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC₅₀ of 62 nM. Alvespimycin (17-DMAG) inhibits the growth of the human cancer cell lines SKBR3 and SKOV3, which overexpress Hsp90 client protein Her2, and causes down-regulation of Her2 as well as induction of Hsp70 consistent with Hsp90 inhibition, for Her2 degradation with EC₅₀ of 8 ± 4 nM and 46 ± 24 nM in SKBR3 and SKOV3 cells, respectively; for Hsp70 induction with EC₅₀ of 4 ± 2 nM and 14 ± 7 nM in SKBR3 and SKOV3 cells, respectively. Compared with the vehicle control, Alvespimycin (17-DMAG) dose-dependent apoptosis (P<0.001 averaged across 24- and 48-hour time points) at concentrations of 50 nM to 500 nM, which represent pharmacologically attainable doses. Similar to many other agents, Alvespimycin (17-DMAG) also demonstrates time-dependent apoptosis (P <0.001, averaged across all doses) in chronic lymphocytic leukemia (CLL) cells with extended exposure from 24 to 48 hours. In addition,Alvespimycin (17-DMAG) is much more potent after 24 and 48 hours of treatment than 17-AAG.

In Vivo: The tumors are grown for two months before the start of i.p. injections every four days over one month with 0, 50, 100 and 200 mg/kg dipalmitoyl-radicicol or 0, 5, 10 and 20 mg/kg Alvespimycin (17-DMAG). Despite sample heterogeneity, the HSP90 inhibitor-treated animals have significantly lower tumour volumes than the vehicle control-treated animals. HSP90 inhibitors have been shown to cause liver toxicity in an animal model of gastrointestinal cancer. Nevertheless, the reduction in tumor size using dipalmitoyl-radicicol is statistically significant at 100 mg/kg, while Alvespimycin (17-DMAG) at either 10 or 20 mg/kg elicits a significant reduction in tumor size.

相关产品：Tamoxifen  |  Tanespimycin  |  Geldanamycin  |  Palmitic acid  |  Rocaglamide  |  VER-155008  |  Arimoclomol maleate  |  PU-WS13  |  Pifithrin-μ  |  MKT-077  |  KNK437  |  KRIBB11  |  Paeoniflorin  |  Retaspimycin Hydrochloride  |  TRC051384  |  ML346  |  Radicicol  |  Teprenone  |  AMP-PCP disodium  |  Ethoxyquin  |  Cucurbitacin D  |  Falcarinol  |  Aminohexylgeldanamycin  |  HS-27  |  3-Phenyltoxoflavin  |  Calenduloside E  |  Geldanamycin-FITC  |  Kongensin A  |  10,11-Dehydrocurvularin

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。