| 货号 | 10543-1mg |
| 描述 | MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity.1 MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer.1 MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.2,3,4 |
| 别名 | AP23573;Deforolimus;Ridaforolimus; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Benjamin, D.,Colombi, M.,Moroni, C., et al. Rapamycin passes the torch: A new generation of mTOR inhibitors. Nature Reviews.Drug Discovery 10(11), 868-880 (2011). 2.Becker, M.A.,Hou, X.,Tienchaianada, P., et al. Ridaforolimus (MK-8669) synergizes with dalotuzumab (MK-0646) in hormone-sensitive breast cancer. BMC Cancer 16(1), 814 (2016). 3.Hernandez, S.F.,Chisholm, S.,Borger, D., et al. Ridaforolimus improves the anti-tumor activity of dual HER2 blockade in uterine serous carcinoma in vivo models with HER2 gene amplification and PIK3CA mutation. Gynecol. Oncol. 141(3), 570-579 (2016). 4.Lamhamedi-Cherradi, S.-E.,Menegaz, B.A.,Ramamoorthy, V., et al. IGF-1R and mTOR blockade: Novel resistance mechanisms and synergistic drug combinations for Ewing sarcoma. J. Natl. Cancer Inst. 108(12), (2016). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 990.2 |
| 分子式 | C53H84NO14P |
| CAS号 | 572924-54-0 |
| 稳定性 | ≥ 2 years |
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