Ridaforolimus (Deforolimus, MK-8669)

Catalog No.S1022 Synonyms: AP23573

Ridaforolimus (Deforolimus, MK-8669) Chemical Structure

Molecular Weight(MW): 990.21

Ridaforolimus (Deforolimus, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 157 In stock
USD 227 In stock
USD 787 In stock

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1 Customer Review

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  Deforolimus for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Ridaforolimus (Deforolimus, MK-8669) purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Ridaforolimus (Deforolimus, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
Targets
mTOR [1]
(HT-1080 cells)
0.2 nM
In vitro

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. [1] 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. [2]

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. [1]

Protocol

Kinase Assay
+ Expand

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 Research
+ Expand
  • Cell lines: Colo205, H1755, H1395, H1666, A549, H157, and H1703 cells
  • Concentrations: Dissolved in ethanol, final concentrations ~ 1 μM
  • Incubation Time: 72-120 hours
  • Method: 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.
    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: 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: Dissolved in ethanol, and diluted in a vehicle of 4% ethanol, 5% Tween 80, and 5% propylene glycol
  • Dosages: ~10 mg/kg
  • Administration: Intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 198 mg/mL (199.95 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 20 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 990.21
Formula

C53H84NO14P

CAS No. 572924-54-0
Storage powder
in solvent
Synonyms AP23573

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02828917 Not yet recruiting de Novo or Restenosis Lesions Medinol Ltd. September 2016 Phase 3
NCT02834806 Not yet recruiting Stenosis Medinol Ltd. August 2016 --
NCT02736344 Recruiting Heart Disease Medinol Ltd. April 2016 Phase 3
NCT01605396 Active, not recruiting Breast Neoplasms Merck Sharp & Dohme Corp. July 2012 Phase 2
NCT01431547 Completed Solid Tumors Merck Sharp & Dohme Corp. February 2012 Phase 1
NCT01431534 Active, not recruiting Solid Tumors Merck Sharp & Dohme Corp. January 2012 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID