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S80076

LY-2584702 (tosylate salt)

MedMol 98%
  • 英文名:
  • LY-2584702 (tosylate salt)
  • 別名:
  • LY2584702 Tosylate; LY-2584702 tosylate salt; 4-{4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl}-1H-pyrazolo[3,4-d]pyrimidine p-toluenesulfonate; LY2584702 tosylate
  • CAS號:
  • 1082949-68-5
  • 分子式:
  • C28H27F4N7O3S
  • 分子量:
  • 617.6177
  • 核磁/質(zhì)譜:
品牌貨號產(chǎn)品規(guī)格價(jià)格(RMB) 庫存(上海) 北京 武漢 南京 數(shù)量計(jì)量單位 加入購物車...
MedMol S80076-1mg 98% ¥190.40元 9 - - - EA 加入購物車
MedMol S80076-2mg 98% ¥258.40元 10 - - - EA 加入購物車
MedMol S80076-5mg 98% ¥442.00元 10 - - - EA 加入購物車
MedMol S80076-10mg 98% ¥646.00元 6 - - - EA 加入購物車
MedMol S80076-25mg 98% ¥1258.00元 6 - - - EA 加入購物車
MedMol S80076-50mg 98% ¥1904.00元 4 - - - EA 加入購物車
源葉(MedMol) S80076-100mg 98% ¥3128.00元 預(yù)計(jì)交期:2-3天 - - - EA 加入購物車
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參考文獻(xiàn)

質(zhì)檢證書(COA)

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  • 提示:詳情請下載說明書。
  • 產(chǎn)品描述: LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM
  • 靶點(diǎn): p70S6K:4 nM (IC50);S6Kinase
  • 體外研究:
    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
  • 體內(nèi)研究:
    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
  • 參考文獻(xiàn):
    1. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75. 2. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50. 3. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.
  • 溶解性: soluble  in  DMSO
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 1.619 ml 8.096 ml 16.191 ml
    5 mM 0.324 ml 1.619 ml 3.238 ml
    10 mM 0.162 ml 0.81 ml 1.619 ml
    50 mM 0.032 ml 0.162 ml 0.324 ml
  • 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。
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