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Deforolimus

Cat. No. M1703

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Deforolimus Structure
Synonym:

Ridaforolimus, AP23573, MK-8669

Size Price Availability
10mg USD 185  USD185 Custom Synthesis
50mg USD 640  USD640 Custom Synthesis
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Quality Control & Documentation
Biological Activity

Deforolimusis (also known as Ridaforolimus, AP23573 and MK-8669) is an investigational targeted and small-molecule inhibitor of the protein mTOR, a protein that acts as a central regulator of protein synthesis, cell proliferation, cell cycle progression and cell survival, integrating signals from proteins, such as PI3K, AKT and PTEN known to be important to malignancy. Deforolimusis blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.

*The compound is unstable in solutions, freshly prepared is recommended

Protocol (for reference only)
Cell Experiment
Cell lines HCT-116, SK-UT-1, HT-1080, SW872, MCF-7, PC-3 cell lines
Preparation method In vitro proliferation assays. Exponentially growing cell lines were plated into two 96-well plates and incubated overnight at 37°C. Twenty-four hours after plating, 1 plate (D1) was aspirated and stored at −80°C. The other plate (D4) was treated with 10-fold serial dilutions of ridaforolimus (1,000 to 0.0001 nmol/L) or vehicle (ethanol). Following 72 hours culture at 37°C, the plates were aspirated and stored at −80°C for proliferation analysis. The D1 and D4 plates were assessed simultaneously for cell growth using the CyQUANT Cell Proliferation Assay Kit (Invitrogen). Doubling time (DT) = [0.301 × (72)/log(day4/day1)]. Doublings = 72/DT. Cell growth rate (%) = doublings ridaforolimus/doublings vehicle × 100. Imax = 100 − cell growth rate (%) at the dose at which maximum inhibition is observed. Imax was used to determine the relative sensitivity of each cell line.
Concentrations 0~1000 n M
Incubation time 72 h
Animal Experiment
Animal models mice bearing PC-3, A549, HCT-116, MCF7, and PANC-1 tumors xenograft model
Formulation diluted in a vehicle of 4% ethanol, 5% Tween 80, and 5% propylene glycol
Dosages 3 and 10 mg/kg (a) daily, 5 continuous days every other week and (b) once weekly
Administration i.p.
Chemical Information
Molecular Weight 990.21
Formula C53H84NO14P
CAS Number 572924-54-0
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Keedy VL. Onco Targets Ther. Treating metastatic soft-tissue or bone sarcomas - potential role of ridaforolimus.

[2] Lush et al. Cancer Chemother Pharmacol. A single supratherapeutic dose of ridaforolimus does not prolong the QTc interval in patients with advanced cancer.

[3] Amato et al. Clin Genitourin Cancer. Safety and Preliminary Efficacy Analysis of the mTOR Inhibitor Ridaforolimus in Patients With Taxane-Treated, Castration-Resistant Prostate Cancer.

[4] Squillace et al. Int J Oncol. Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models.

[5] Stroh et al. Cancer Chemother Pharmacol. The effect of multiple doses of rifampin and ketoconazole on the single-dose pharmacokinetics of ridaforolimus.

[6] Berk et al. Cancer Chemother Pharmacol. Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial.

[7] Rivera VM, et al. Mol Cancer Ther. Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens.

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Keywords: Deforolimus, Ridaforolimus, AP23573, MK-8669 supplier, mTOR, inhibitors, activators

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