Everolimus

• 产品编号：CST-12017S      品牌：CST       原厂货号：12017S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

Everolimus以冻干粉形式提供。可将1 mg冻干粉重悬于1.04 ml DMSO制成1 mM贮存液。工作浓度和处理时间的长短取决于预期效果，但通常建议使用10-100 nM预处理0.5-1 hr，然后再加刺激物或结合不同的处理时间单独使用，最长可达24hr。可溶解于DMSO或乙醇，浓度为100 mg/ml；水中溶解度极差，最大溶解度为~1-10 µM。Everolimus，也被称为RAD001，是雷帕霉素的一种免疫抑制剂类似物。Everolimus可与FKBP12形成一种在FK506竞争结合试验中IC50 = ~2 nM的复合物（1,2）。该复合物随后可以结合并抑制mTORC1 (3)。研究表明everolimus处理细胞可以导致mTOR下游靶标的去磷酸化（4-7）、抑制VEGF和 bFRF刺激的HUVE增殖（6）以及低氧诱导HIF-1蛋白水平的降低（7）。

原厂资料：

Molecular Characterization

C53H83NO14

Purity

>99%

Directions for Use

Everolimus is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 1 mg in 1.04 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 10-100 nM either as a pretreatment for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO or ethanol at 100 mg/ml; very poorly soluble in water with maximum solubility ~1-10 µM.

Background

Everolimus, also known as RAD001, is an immunosuppressant analog of rapamycin. Everolimus forms a complex with FKBP12 with an IC50 = ~2 nM in FK506 competitive binding assays (1,2), and this complex then binds to and inhibits mTORC1 (3). Studies have shown that everolimus treatment of cells can lead to the dephosphorylation of mTOR downstream targets (4-7), inhibition of VEGF- and bFRF-stimulated proliferation in HUVE cells (6), and reduction of hypoxia-induced HIF-1 protein levels (7).

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated.
Protect from light. In lyophilized form, the chemical is stable for
24 months. Once in solution, use within 3 months to prevent loss
of potency. Aliquot to avoid multiple freeze/thaw cycles.