| 品牌 | 貨號(hào) | 產(chǎn)品規(guī)格 | 價(jià)格(RMB) | 庫(kù)存（上海） | 北京 | 武漢 | 南京 | 購(gòu)買數(shù)量 |
|---|---|---|---|---|---|---|---|---|
| MedMol | S80076-1mg | 98% | ￥150.00元 | 9 | - | - | - |
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| MedMol | S80076-2mg | 98% | ￥240.00元 | 10 | - | - | - |
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| MedMol | S80076-5mg | 98% | ￥442.00元 | 10 | - | - | - |
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| MedMol | S80076-10mg | 98% | ￥646.00元 | 6 | - | - | - |
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| MedMol | S80076-25mg | 98% | ￥1258.00元 | 6 | - | - | - |
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| MedMol | S80076-50mg | 98% | ￥1904.00元 | 4 | - | - | - |
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| 源葉(MedMol) | S80076-100mg | 98% | ￥3128.00元 | 預(yù)計(jì)交期：2-3天 | - | - | - |
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| 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 | ||||||||||||||||||||
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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 |
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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 |
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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. |
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| 溶解性： soluble in DMSO | ||||||||||||||||||||
| 保存條件： -20℃ | ||||||||||||||||||||
配置溶液濃度參考：
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| 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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