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Ridaforolimus (Deforolimus, MK-8669)
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
货号 | CAS号 | 操作 |
---|---|---|
D126066-100mg | 572924-54-0 | 询价 |
D126066-10mg | 572924-54-0 | 询价 |
D126066-50mg | 572924-54-0 | 询价 |
D126066-5mg | 572924-54-0 | 询价 |
产品介绍
属性
溶解性 | DMSO ≥196mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
存贮条件 | 储存温度-20°C |
描述
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 |
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途