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CAS No. : 1082949-68-5
MCE 国际站: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 | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Targeted Diversity Library | Highly Selective Inhibitors Library | SL 0101-1 | RSK2-IN-3 | Hu7691 free base | AT13148 | CKI-7 free base | FMK-MEA | LY-2584702 hydrochloride | S6K1-IN-1 | Pluripotin | AT7867 | DD1 | AD57 | AD80 | PF-4708671 | MBM-55S | Quercitrin | M2698 | SM1-71 | BI-D1870 | S6 Kinase Substrate Peptide 32 | LJH685 | BIX 02565 | RSK4-IN-1 | Sodium Salicylate | Bisindolylmaleimide V | BRD7389
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