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。

Retaspimycin Hydrochloride

CAS No. : 857402-63-2

MCE 站：Retaspimycin Hydrochloride

产品活性：Retaspimycin Hydrochloride是有效的 Hsp90 抑制剂，EC₅₀ 为119 nM。

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

作用靶点：HSP

In Vitro: Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. The IC₅₀s for the inhibition of reporter gene activity by Retaspimycin are 196±56 nM in U266 and 472±177 nM in MM.1s for UPRE-luc activity and 213±140 nM for the ERSE-driven activity in MM.1s cells. Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC₅₀ of 237 nM, consistent with the reporter-gene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC₅₀ between 300 nM and 1 μM. Incubation of Retaspimycin (IPI-504) potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment.

In Vivo: Retaspimycin (IPI-504) and Trastuzumab independently induce tumor regression of Trastuzumab-sensitive BT474 cell-derived xenografts. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin (100 mg/kg) as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts. The combination is not significantly superior to Retaspimycin used as a single agent.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Endoplasmic Reticulum Stress Compound Library  |  Pyroptosis Compound Library  |  Cytoskeleton Compound Library  |  Tamoxifen  |  Tanespimycin  |  Geldanamycin  |  Palmitic acid  |  Rocaglamide  |  VER-155008  |  Arimoclomol maleate  |  PU-WS13  |  Pifithrin-μ  |  MKT-077  |  KNK437  |  KRIBB11  |  Paeoniflorin  |  TRC051384  |  ML346  |  Radicicol  |  Tepre  |  AMP-PCP disodium  |  Ethoxyquin  |  Cucurbitacin D  |  Falcarinol  |  Aminohexylgeldanamycin  |  HS-27  |  3-Phenyltoxoflavin  |  Alvespimycin  |  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。