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()
    TIC10 (imipridone, ONC201, NSC350625)
    TIC10 (imipridone, ONC201, NSC350625)

    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 #: V0172
    CAS号码 #: 1616632-77-9纯度 ≥98%

    Description: TIC10 (ONC-201, NSC-350625), an imipridone compound, is a novel, potent, orally bioavailable, brain/BBB penetrant, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer with potential anticancer activity. It was initially developed in the 1970s as an anti-seizure agent which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can inactivate Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. TIC10 is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10. 

    References:Cancer Res. 2015 Apr 15;75(8):1668-74; Sci Transl Med. 2013 Feb 6;5(171):171ra17.

    Related CAS #1616632-77-9 (free base)1638178-82-1 (HCl); 41276-02-2 (TIC10 analog); 1777785-71-3 (HBr)   2007141-57-1 (2HBr)  41276-02-2 (TIC10 isomer)

    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)386.49
    FormulaC24H26N4O
    CAS No.1616632-77-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 77 mg/mL (199.2 mM) 
    Water: <1 mg/mL
    Ethanol:  77 mg/mL (199.2 mM) 
    Other info

    Chemical Name: 7-benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one

    SMILES Code: O=C1N(CC2=CC=CC=C2C)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4

    Synonymimipridone; NSC350625; NSC-350625; NSC 350625; TIC10; TIC 10; ONC201; ONC 201; ONC-201; TIC-10; TRAIL inducing compound 10;  


    • 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 Assay: TIC10 transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their micro-environment to enhance the concentrations of the endogenous tumor suppressor TRAIL. TIC10 also causes a down-regulation of the total expression of ERK.

     

    Cell Assay: TIC10 causes a dose-dependent increase in TRAIL mRNA and induces TRAIL protein localization on the cell surface of several cancer cell lines in a p53-independent manner. TIC10 has broad-spectrum activity against multiple malignancies in vitro and induces an increase in sub-G1 DNA content suggestive of cell death in TRAIL-sensitive HCT116 p53−/− cells, but does not alter the cell cycle profiles of normal fibroblasts at equivalent doses. TIC10 decreases the clonogenic survival of cancer cell lines and spares normal fibroblasts. TIC10 increases the percentage of sub-G1 DNA in cancer cells in a p53-independent and Bax-dependent manner, as previously reported for TRAIL-mediated apoptosis. TIC10-induced TRAIL up-regulation is Foxo3a-dependent, which also up-regulates TRAIL death receptor DR5 among other targets, potentially allowing for sensitization of some TRAIL-resistant tumor cells. TIC10 inactivates kinases Akt and extracellular signal–regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL.

    In Vivo

    TIC10 and TRAIL treatment causes tumor regression in the HCT116 p53−/− xenograft to a comparable extent when both are administered as multiple doses. TIC10 also induces regression of MDA-MB-231 human triple-negative breast cancer xenografts, whereas TRAIL-treated tumors progressed. In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progresses after a single dose. A single dose of TIC10 also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for TIC10. TIC10 causes tumor-specific cell death by TRAIL-mediated direct and bystander effects. TIC10 is an effective antitumor agent against orthotopic human glioblastoma multiforme tumors.

    Animal model

    Female athymic nu/nu mice

    Formulation & Dosage

    Dissolved in DMSO;  25, 50, 100 mg/kg; p.o./i.p.

    References

    [1] Allen JE, et al. Sci Transl Med, 2013, 5(171), 171ra17.

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

    TIC10

    TIC10 is a small molecule that induces TRAIL independent of p53. Sci Transl Med, 2013, 5(171), 171ra17.



    TIC10

    TIC10 induces TRAIL in tumor and normal cells.

    TIC10

    TIC10 is effective as an antitumor agent in GBM.


    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*
      • *
      • 邮箱*
      • *
      • 详细说明:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved