我的购物车
购物车中还没有商品,赶紧选购吧!
  • 产品名称
  • 规格
  • 数量
  • 总价
    已选择商品 : 0 总计 : 结账()
    LY2584702 Tosylate (LYS-6K2)
    LY2584702 Tosylate (LYS-6K2)

    售价:
    市场价:

    产品仅用于科学研究,不针对患者销售
    数量: - + 件(库存件)
    InvivoChem目录号 #: V0241
    CAS号码 #: 1082949-68-5 纯度 ≥98%

    Description: LY2584702 Tosylate (also known as LYS6K2), the tosylate salt of LY2584702, is a selective, orally bioavailable, and ATP-competitive p70S6K (ribosomal p70 S6 kinase) inhibitor with potential antitumor activity. It inhibits p70S6K with an IC50 of 4 nM. LY2584702 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo by inhibiting ribosomal protein S6 Kinase (p70S6K), and preventing phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation. 

    References: Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.

    Related CAS: 1082949-67-4 (free base); 1082948-81-9 (HCl); 1082949-68-5 (tosylate) 

    Customer Validation
    世界名校的官方供应商
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    相关产品
    顾客使用 InvivoChem产品发表科研文献
    • 产品理化性质和储存条件
    • 实验参考方法
    • 质控文件
    • 生物活性
    • 顾客评价

    Molecular Weight (MW)

    617.62

    Formula

    C28H27F4N7O3S

    CAS No.

    1082949-68-5 (tosylate)

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 7 mg/mL (11.3 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    SMILES Code

    CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3

    Synonyms

    LYS6K2 tosylate; LY2584702; LY 2584702; LY-2584702; LYS-6K2; LYS 6K2; LY2584702 tosylate

    Chemical Name: 4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine 4-methylbenzenesulfonate

    SMILES Code: CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3.OS(=O)(C6=CC=C(C)C=C6)=O

    Exact Mass: 445.1638 


    • 摩尔计算器
    • 稀释计算器
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2

    In Vitro

    In vitro activity: In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus.

     

    Kinase Assay: LY2584702 Tosylate (also known as LYS6K2) is a novel, selective, orally bioavailable, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. 

     

    Cell Assay: LY-2584702 is fully dissolved in 20 mL 10% DMSO and reserved at -80°C. When conducted the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol and 30% PEG400 to reach different DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. Cell Counting Kit-8 (CCK-8) is used to measure the cells proliferation in vitro. Cell lines A549 and SK-MES-1 treated by LY-2584702 for 24 h with different concentrations are seeded in 96-well plates at a density of 5×103 per well, with six repeats. DMSO treated, or in other words, the concentration of LY-2584702 of 0 is used as negative control. Cells absorbance at 450 nm is detected every 24 h after seeding to measure the proliferative activities[

    In Vivo

    LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.

    Animal model

    Mice

    Formulation & Dosage

    Dissolved in 0.25% Tween-80 and 0.05% antifoam;12.5 mg/kg twice daily, oral

    References

    Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LY2584702 Tosylate

    Protein expression of RPS6KB1, p-RPS6KB1, rpS6 and p-rpS6 after the treatment by various LY2584702 concentrations for 24 h.  2017 Aug 9;12(8):e0182891.

    LY2584702 Tosylate

    Proliferation alteration of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702 (CCK-8 analysis).  2017 Aug 9;12(8):e0182891.

    LY2584702 Tosylate

    Cell cycle distribution of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702.  2017 Aug 9;12(8):e0182891.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      你的资料在我们这儿很安全* 必填项。
      InvivoChem的所有产品仅用于作科学研究,不面向患者销售
      电话:020-31522723
      QQ:463611831
      电子邮箱: sales@invivochem.net
      获得最新产品资讯、折扣和优惠
      • 姓名*
      • *
      • 邮���*
      • *
      • 详细说明:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved