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    Ridaforolimus (Deforolimus, MK8669, AP23573)
    Ridaforolimus (Deforolimus, MK8669,  AP23573)

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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 #: V0184
    CAS #: 572924-54-0Purity ≥98%

    Description: Ridaforolimus (also known as deforolimus, AP-23573; MK-8669) is a novel, potent, investigational and selective mTOR inhibitor with significant antitumor effects. It inhibits mTOR with an IC50 of 0.2 nM in HT-1080 cell line; while Ridaforolimus is not classified as a prodrug, it inhibits mTOR and FKBP12 similarly to that of rapamycin. mTOR is a protein that acts as a central regulator of protein synthesis, cell proliferation, cel l cycle progression and cell survival, integrating signals from proteins, such as PI3K, AKT and PTEN known to be important to malignancy. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis. It has had promising results in a clinical trial for advanced soft tissue and bone sarcoma.

    References: Mol Cancer Ther. 2011 Jun;10(6):1059-71; Cancer Res. 2012 Sep 1;72(17):4483-93.

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    Molecular Weight (MW)

    990.21

    Formula

    C53H84NO14P

    CAS No.

    572924-54-0

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 198 mg/mL (200 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

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    Synonyms

    AP23573, Deforolimus, MK-8669; AP23573; AP 23573; AP-23573; MK8669; MK 8669; MK-8669; Deforolimus, Ridaforolimus


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    In Vitro

    Kinase Assay: Cell based target inhibition: HT-1080 cells are treated with increasing concentrations of Deforolimus (0-100 nM) for 2 hours, prior to harvest. Cellular lysates are extracted in denaturing lysis buffer, resolved on SDS-PAGE and transferred to PVDF membranes. After blocking, membranes are incubated with primary antibodies for 1 hour, followed by appropriate HRPconjugated secondary antibodies for 1 hour at room temperature. Immunoreactive proteins are detected using enhanced chemiluminescence and autoradiography performed by exposure to X-ray film. IC50 is determined from the inhibition of levels of phosphorylated ribosomal protein S6 (p-S6) and 4E-BP1 (p-4E-BP1). 

     

    Cell Assay: Cells (Colo205, H1755, H1395, H1666, A549, H157, and H1703 cells) are seeded at 2-3 × 104/mL, and serial dilutions of Deforolimus are added after 2 hours, for at least three cell doublings (72-120 hours). Deforolimus effects are measured using the CellTiter 96 Aqueous nonradioactive cell proliferation assay and Sulforhodamine B assays. For Deforolimus, growth effects are described as IC30 because rapamycin and its derivatives do not significantly impede cell proliferation.

    Treatment of HT-1080 cells with Deforolimus induces a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. Deforolimus displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM. Deforolimus potently and selectively inhibits VEGF production in a dose-dependent manner. Deforolimus treatment significantly induces growth suppression in human NSCLC cell lines with IC30 values of 2.45-8.83 nM, with the exception of H157 with IC30 of >20 nM. Deforolimus treatment (2.8-5.9 nM) significantly dephosphorylates p70S6KThr389 in A549, H1703 and H157 cells, except H1666 that may express a resistant variant of mTORC1, and causes increased phosphorylation of pAKTser473 and pAKTThr308 in A549 and H1703 cells. Deforolimus in combination with the MEK inhibitors, CI-1040 or PD0325901 exhibits dose-dependent synergism in lung cancer cell lines, which is associated with the suppression of proliferation rather than enhancement of cell death, involving the inhibition of ribosomal biogenesis by 40% within 24 hours and a decreased polysome/monosome ratio.

    In Vivo

    Administration of Deforolimus exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts in a dose-dependent manner, and inhibits mTOR signaling in in SK-LMS-1 xenograft model associated with inhibition of tumor growth.

    Animal model

    Male and female athymic NCr-nu mice with xenografts established by subcutaneous implantation of PC-3, A549, HCT-116, MCF7, PANC-1 and SK-LMS-1 tumors.

    Formulation & Dosage

    Formulated in  ethanol, and diluted in a vehicle of 4% ethanol, 5% Tween 80, and 5% propylene glycol; 10 mg/kg; i.p. injection.

    References

    Mol Cancer Ther. 2011 Jun;10(6):1059-71; Cancer Res. 2012 Sep 1;72(17):4483-93.


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

    Ridaforolimus (Deforolimus, MK-8669)

    Ridaforolimus attenuates mTOR signaling, resulting in cell shrinkage, cytostatic, and metabolic effects. Mol Cancer Ther, 2011, 10(6), 1059-1071.

    Ridaforolimus (Deforolimus, MK-8669)

    Ridaforolimus treatment inhibits tumor cell proliferation independent of PTEN status or AKT activation.

    Ridaforolimus (Deforolimus, MK-8669)

    In vivo activity and efficacy of ridaforolimus. Mol Cancer Ther, 2011, 10(6), 1059-1071.


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