| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| E409231-1ml |
1ml |
现货  |
|
| 别名 | 依维莫司 (RAD001) |
|---|---|
| 英文别名 | SDZ-RAD |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Everolimus (RAD001) |
| 生化机理 | 依维莫司（RAD001，SDZ-RAD）是一种 FKBP12 的 mTOR 抑制剂，在无细胞试验中的 IC50 值为 1.6-2.4 nM。依维莫司可诱导细胞凋亡和自噬，抑制肿瘤细胞增殖。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | FK506 结合蛋白 1A 抑制剂 |
| 产品介绍 |
Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，IC50为1.6-2.4 nM。An immunosuppresive inhibitor of FRAP (mTOR). Information
Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. Everolimus also shows antiangiogenic/vascular effects in VEGF-induced HUVEC proliferation with IC50 of 0.12 nM and bFGF-induced HUVEC proliferation with IC50 of 0.8 nM, respectively. A recent study shows that Everolimus shows a dose-dependent inhibitory effects on both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells with IC50 of 156 nM in total cells of primary breast cancer cells and 71 nM in total cells of BT474 cells. In addition, combination treatment with Everolimus and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %. In vivo Everolimus (0.1 to 10 mg/kg) dose-dependently inhibits growth of the primary (ear) and lymph node metastases of B16/BL6 melanoma, with decreased total number of vessels and reduced mature vessels. In a xenograft animal model of BT474 stem cells, Everolimus shows significant reductions in mean tumor sizes (590.6 mm3), compared to the control group with a tumor size of 698 mm3. Furthermore, combination treatment with Everolimus and trastuzumab significantly decreases the xenograft tumor size (410.8 mm3) more than Everolimus treatment alone. cell lines： Concentrations：0.001-10 μM Incubation Time：24 hours Powder Purity:≥97% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1CC(CCC1OCCO)CC(C)C2CC(=O)C(C)\C=C(C)\C(O)C(OC)C(=O)C(C)CC(C)/C=C/C=C/C=C(C)/C(CC3CCC(C)C(O)(O3)C(=O)C(=O)N4CCCCC4C(=O)O2)OC |
| 分子量 | 958.22 |
| concentration (1mL in DMSO) | 9.0-11.0（mmol/L） |
|---|---|
| NMR Spectrum 1H | conforms to structure |
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