ridaforolimus-deforolimus-mk-8669

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.