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    TIC10 Analogue (ONC-201 isomer)
    TIC10 Analogue (ONC-201 isomer)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0168
    CAS #: 41276-02-2Purity ≥98%

    Description: TIC10 Analogue (ONC201 isomer) is an analog/isomer of TIC10 and the 'inactive form' of TIC10. It was structurally similar to TIC10 but is inactive and did not decrease the viability of cancer cells.

    References:Sci Transl Med. 2013 Feb 6;5(171):171ra17.

    Related CAS #: 1616632-77-9 (free base); 1638178-82-1 (HCl)   

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    Molecular Weight (MW)386.49
    FormulaC24H26N4O
    CAS No.41276-02-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 11 mg/mL (28.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoSynonym: TIC10 isomer; TIC 10 isomer; TIC10 isomer; ONC201 isomer; ONC 201 isomer; ONC201 isomer.

    InChi Key: RSAQARAFWMUYLL-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H26N4O/c1-18-7-5-6-10-20(18)16-28-22-11-13-26(15-19-8-3-2-4-9-19)17-21(22)23(29)27-14-12-25-24(27)28/h2-10H,11-17H2,1H3

    SMILES Code: O=C1C(CN(CC2=CC=CC=C2)CC3)=C3N(CC4=CC=CC=C4C)C5=NCCN15

    Chemical Name7-benzyl-10-(2-methylbenzyl)-2,3,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[4,3-d]pyrimidin-5(10H)-one


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    In Vitro

    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; i.p./p.o.

    References

    Sci Transl Med. 2013 Feb 6;5(171):171ra17.

     


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

    TIC10 Analogue


    TIC10 Analogue

    TIC10 induces TRAIL in tumor and normal cells.

    TIC10 Analogue

    TIC10 is effective as an antitumor agent in GBM.



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