1. PI3K/Akt/mTOR
    Autophagy
  2. mTOR
    Autophagy
  3. Deforolimus

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

Cat. No.: HY-50908 Purity: 98.46%
Handling Instructions

Deforolimus (AP23573; 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.

Deforolimus Chemical Structure

Deforolimus Chemical Structure

CAS No. : 572924-54-0

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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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    Description

    Deforolimus (AP23573; 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.

    IC50 & Target[1]

    mTOR

     

    In Vitro

    Treatment of HT-1080 fibrosarcoma cells with deforolimus 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 deforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of deforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Deforolimus 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].

    In Vivo

    Deforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Deforolimus 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].

    Clinical Trial
    Molecular Weight

    990.21

    Formula

    C₅₃H₈₄NO₁₄P

    CAS No.

    572924-54-0

    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.

      Deforolimus is dissolved in 1% DMSO in sunflower seed oil[2].

    References
    Cell Assay
    [1]

    Cells are treated with 10-fold serial dilutions of deforolimus (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. Deforolimus, 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

    Purity: 98.46%

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    Product name:
    Deforolimus
    Cat. No.:
    HY-50908
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