2. PI3K/Akt/mTOR
    Autophagy
    Anti-infection
  3. mTOR
    Autophagy
    Bacterial
  4. Ridaforolimus

Ridaforolimus  (Synonyms: MK-8669; Deforolimus; AP23573)

Cat. No.: HY-50908 Purity: ≥98.0%
COA Handling Instructions

Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.

For research use only. We do not sell to patients.

Ridaforolimus Chemical Structure

Ridaforolimus Chemical Structure

CAS No. : 572924-54-0

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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Ridaforolimus purchased from MCE. Usage Cited in: Cell Metab. 2018 Jan 9;27(1):118-135.e8.  [Abstract]

    Inhibiting mTORC1 activity by intraperitoneally injecting DSS-treated C57BL/6 mice with Deforolimus or Torin 1 every other day also results in significant body weight loss compared with controls.

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    mTOR mTORC1 mTORC2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells[1].

    IC50 & Target[1]

    mTOR

     

    In Vitro

    Treatment of HT-1080 fibrosarcoma cells with Ridaforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50s of 0.2 and 5.6 nM, respectively, and EC50s of 0.2 and 1.0 nM, respectively. In HT-1080 cells, the EC50 for inhibition of cell proliferation (0.5 nM) is similar to the EC50s for inhibition of S6 and 4E-BP1 phosphorylation. Exposure to Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    Ridaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    990.21

    Appearance

    Solid

    Formula

    C53H84NO14P
    CAS No.
    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 44 mg/mL (44.44 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0099 mL 5.0494 mL 10.0989 mL
    5 mM 0.2020 mL 1.0099 mL 2.0198 mL
    10 mM 0.1010 mL 0.5049 mL 1.0099 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (2.52 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (2.52 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: ≥98.0%

    COA (261 KB) HNMR (250 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells are treated with 10-fold serial dilutions of Ridaforolimus (1,000 to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37°C, the plates are aspirated and stored at -80°C for proliferation analysis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Animals selected with tumors in the proper size range are assigned to various treatment groups. Ridaforolimus, at dosages of 3 and 10 mg/kg, is administered i.p. on 2 different treatment schedules: (a) daily, 5 continuous days every other week and (b) once weekly. The control group is untreated[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • 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.

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    Keywords:

    Ridaforolimus572924-54-0MK-8669 Deforolimus AP23573MK8669MK 8669AP23573AP 23573AP-23573mTORAutophagyBacterialMammalian target of RapamycinInhibitorinhibitorinhibit

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