产品描述
| 溶解性 | DMSO ≥196mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| 存贮条件 | 储存温度-20°C |
| 应用 | A selective FRAP (mTOR) inhibitor |
| 产品介绍 | Ridaforolimus (Deforolimus, MK-8669)是一种选择性的mTOR抑制剂，IC50为0.2 nM；对mTOR信号通路的抑制作用及与FKBP12结合能力和Rapamycin接近。 |
| 备注 | Ridaforolimus (Deforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. |
| 生化机理 | Deforolimus is a selective FRAP (mTOR) inhibitor (IC50 of 0.2 nM), used to treat HT-1080 cells induces a dose-dependent inhibition of both S6 and 4E-BP1 phosphorylation, 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. Ridaforolimus shows antiproliferative activity a variety of cell lines with EC50 of 0.2-2.3 nM. Ridaforolimus is a potent and selective inhibitor of VEGF production in a dose-dependent manner. Ridaforolimus treatment causes 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. Ridaforolimus treatment causes dephosphorylation of 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. |
| 别名 | AP23573;药雷帕霉素;MK 8669; 42-(二甲基亚膦酰)雷帕霉素;AP23573; MK-8669; Ridaforolimus; AP 23573; MK 8669; AP-23573; MK8669;42-(Dimethylphosphinate)rapamycin |
