2. Apoptosis
  3. TNF Receptor Apoptosis
  4. Dordaviprone

Dordaviprone (TIC10) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. Dordaviprone can cross the blood-brain barrier.

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CAS No. : 1616632-77-9

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Based on 10 publication(s) in Google Scholar

Dordaviprone Related Antibodies

Top Publications Citing Use of Products

    Dordaviprone purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 10;9(15):12020-12034.  [Abstract]

    WB detection of the total and phosphorylated ERK1/2, LC3B, p62, ATG5, ATG7 levels in the PC9/GR and HCC827/GR cells cultured in the four treatment conditions. 20 μM TIC10 treatment decreases the expression of LC3B-II, but increases the expression of p62 in both cells.

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    TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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    Description

    Dordaviprone (TIC10) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. Dordaviprone can cross the blood-brain barrier[1].

    IC50 & Target[1]

    TRAIL

     

    In Vitro

    Dordaviprone transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier[1].
    Dordaviprone induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of Dordaviprone[1].
    Dordaviprone 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[1].
    Dordaviprone 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[1].
    Dordaviprone also causes a down-regulation of the total expression of ERK[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dordaviprone Related Antibodies
    In Vivo

    In DLD-1 colon cancer xenografts, Dordaviprone induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progress after a single dose. A single dose of Dordaviprone 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 Dordaviprone. Titration of a single oral dose of Dordaviprone in the HCT116 xenograft model reveals sustained antitumor efficacy at 25 mg/kg. Exposure to oral Dordaviprone at 25 mg/kg weekly for 4 weeks in immunocompetent mice does not cause any changes in selected serum chemistry markers. The same oral dosing schedule is applied to Eμ-myc transgenic mice, which spontaneously develop meta-static lymphoma from weeks 9 to 12 of age, and Dordaviprone significantly (P=0.00789) prolongs the survival of these mice by 4 weeks[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Essai clinique
    Masse moléculaire

    386.49

    Formule

    C24H26N4O
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1N(CC2=CC=CC=C2C)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvant et solubilité
    In Vitro: 

    DMSO : 9.38 mg/mL (24.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5874 mL 12.9369 mL 25.8739 mL
    5 mM 0.5175 mL 2.5874 mL 5.1748 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Pureté et documentation

    Purity: 99.89%

    SDS (396 KB)

    COA (247 KB) LCMS (93 KB)

    Instruction de manipulation (2659 KB)
    Références
    Test cellulaire
    [1]

    Floating and adherent cells are analyzed on a Coulter-Beckman Elite Epics cytometer. For surface TRAIL experiments, adherent cells are harvested by brief trypsinization, fixed in 4% paraformaldehyde in phosphate-buffered saline (PBS) for 20 min, incubated with an anti-TRAIL antibody at 1:250 overnight, washed and incubated with anti-rabbit Alexa Fluor 488 for 30 min, and analyzed. Cells are gated on forward and side scatter to eliminate debris and dead cells from the analysis. Surface TRAIL data are expressed as median fluorescence intensity relative to that of control samples unless indicated otherwise. Surface DR5 is analyzed similarly with an antibody from Imgenex. For sub-G1content and cell cycle profile analysis, all cells are pelleted and ethanol-fixed, followed by staining with propidium iodide in the presence of RNase. Cell viability assays are carried out in 96-well black-walled clear-bottom plates with CellTiter-Glo[1].

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Administration animale
    [1]

    Mice[1]
    For subcutaneous xenografts, 4- to 6-week-old female athymic nu/nu mice are inoculated with 1×106 cells (2.5×106 for T98G) of the indicated cell lines in each rear flank as a 200-μL suspension of 1:1 Matrigel (BD)/PBS. All subcutaneous tumors are allowed to establish for 1 to 4 weeks after injection until reaching a volume of ~125 mm3 before treatment initiation. All intraperitoneal and intravenous injections are given at a total volume of 200 μL. Oral formulations of Dordaviprone are administered by oral gavage and given as a 200 μL suspension containing 20% Cremophor EL, 10% DMSO, and 70% PBS. Tumors are monitored with digital calipers at indicated time points. All subcutaneous tumors are allowed to establish for 1-4 weeks post-injection until reaching a volume of ~125 mm3 before treatment initiation. Relief of tumor burden is monitored for 3 weeks after disappearance of the tumor and confirmed by visual inspection after euthanasia.

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Références

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5874 mL 12.9369 mL 25.8739 mL 64.6847 mL
    5 mM 0.5175 mL 2.5874 mL 5.1748 mL 12.9369 mL
    10 mM 0.2587 mL 1.2937 mL 2.5874 mL 6.4685 mL
    15 mM 0.1725 mL 0.8625 mL 1.7249 mL 4.3123 mL
    20 mM 0.1294 mL 0.6468 mL 1.2937 mL 3.2342 mL
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    Dordaviprone Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dordaviprone1616632-77-9TIC10 ONC-201TIC 10TIC-10ONC201ONC 201ONC-201TNF ReceptorApoptosisTumor Necrosis Factor ReceptorTNFRInhibitorinhibitorinhibit

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