简介: 货 号:LC1-R-7040 名 称:42-(二甲基亚膦酰)雷帕霉素;雷帕霉素衍生物;药雷帕霉素 别 名:Ridaforolimus C A S :572924-54-0 分子量:990.21 分子式:C53H84NO14P 纯 度:HPLC/TLC:>99% 说 明:Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A 文 献:Ridaforolimus (the name has been changed from "deforolimus") is an immunosuppressant and a novel small-molecule inhibitor of the protein mammalian target of rapamycin (mTOR). Ridaforolimus inhibits cancer cell growth, cell division, metabolism, and angiogenesis by blocking mTOR. Mahalingam, D., et al. "Targeting the mTOR pathway using deforolimus in cancer therapy." Future Oncol. 5: 291-303 (2009).Ridaforolimus had an antitumor activity in >85% of patients with advanced solid tumors. Rivera, V.M., et al. "Pharmacodynamic study of skin biopsy specimens in patients (pts) with refractory or advanced malignancies following administration of AP23573, an mTOR inhibitor." J. Clin. Oncol. 23: 3033 (2005).Ridaforolimus has low toxicity profiles and promising clinical efficacy in patients with advanced sarcomas. Chawla, S.P., et al. "Updated results of a phase II trial of AP23573, a novel mTOR inhibitor, in patients (pts) with advanced soft tissue or bone sarcomas." J. Clin. Oncol. 24: 9505 (2006).The level of phosphorylated S6 ribosomal protein expression was a marker of early tumor response to ridaforolimus. Iwenofu, O.H., et al. "Phospho-S6 ribosomal protein: a potential new predictive sarcoma marker for targeted mTOR therapy." Mod. Pathol. 21: 231-237 (2008).MEK inhibitors in combination with the mTOR inhibitor, rapamycin or its analogue ridaforolimus, exhibited synergism in human lung cancer cell lines by inhibiting proliferation rather than promoting cell death. Legrier, M.E., et al. "Targeting protein translation in human non small cell lung cancer via combined MEK and mammalian target of rapamycin suppression." Cancer Res. 67: 11300-11308 (2007).