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。

LY-2584702 tosylate salt

CAS No. : 1082949-68-5

MCE 站：LY-2584702 tosylate salt

产品活性：LY-2584702 tosylate salt 是一种 ATP 竞争性的选择性 p70S6K 抑制剂，IC₅₀ 为 4 nM。LY-2584702 抑制 S6K1 的 IC₅₀ 为 2 nM。

研究领域：MAPK/ERK Pathway

作用靶点：Ribosomal S6 Kinase (RSK)

In Vitro: LY-2584702 (LY2584702) inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC₅₀ of 0.1-0.24 μM. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 (LY2584702) is 2 nM. For pS6 inhibition in cells, the IC₅₀=100 nM. LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC₅₀=58-176 nM). LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner. Proliferation of A549 is significantly inhibited by LY-2584702 (LY2584702) treating over 24 h at 0.1 μM (P<0.05); and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05). Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549.

In Vivo: LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glutamine Metabolism Compound Library  |  PF-4708671  |  Carnosol  |  Pluripotin  |  LJH685  |  Sodium Salicylate  |  LJI308  |  Quercitrin  |  SL 0101-1  |  CKI-7 free base  |  AT7867 dihydrochloride  |  BRD7389  |  Eudesmin  |  SM1-71

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。