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Everolimus (Synonyms: 依维莫司; RAD001; SDZ-RAD) 纯度: 99.74%
Everolimus (RAD001) 是一种 Rapamycin 的衍生物,也是一种有效的,选择性的和口服活性的 mTOR1 抑制剂。Everolimus 与 FKBP-12 结合可产生免疫抑制复合物。Everolimus 抑制肿瘤细胞增殖并诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Everolimus 具有有效的免疫抑制和抗癌活性。
Everolimus Chemical Structure
CAS No. : 159351-69-6
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥854 | In-stock | |
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10 mg | ¥810 | In-stock | |
50 mg | ¥2743 | In-stock | |
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Everolimus 相关产品
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生物活性 |
Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits the Ser/Thr kinase, mTOR[1]. In both the sensitive murine B16/BL6 melanoma (IC50, 0.7 nM) and the insensitive human cervical KB-31 (IC50, 1,778 nM), antiproliferative concentrations of Everolimus results in total dephosphorylation of S6K1 and the substrate S6 and a shift in the mobility of 4E-BP1, which is indicative of a reduced phosphorylation status[3]. Everolimus exhibits a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells, albeit with different degrees of growth inhibition. Compare with the total cells, Everolimus is less effective in growth inhibition in the stem cells at all tested concentrations (P<0.001). The IC50 values of Everolimus for BT474 and the primary CSCs are 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC50 values for their corresponding total cells, respectively[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Everolimus is orally active in both mice and rats, producing an antitumor effect that is characterized by dramatic reduction in tumor growth rates as opposed to producing tumor regressions. In the rat CA20498 model, daily treatment with Everolimus (0.5 or 2.5 mg/kg) dose-dependently inhibits growth, and intermittent dosing using a higher dose of 5 mg/kg (once or twice per week) also shows similar antitumor efficacy. Inhibition by Everolimus is characterized by sustained suppression rather than regression and is not associated with any body weight loss[1]. The effect of Everolimus treatment (0.1-10 mg/kg/d) is selective and differ from the effects of PTK/ZK (100 mg/kg). With either growth factor, Everolimus dose-dependently increases the hemoglobin content (convert to blood equivalents and indicative of the number of vessels as well as vascular leakiness) but reduces the Tie-2 content (number of endothelial cells indicative of the number of vessels) and this is significant for VEGF stimulation but not bFGF stimulation. The pharmacokinetics of Everolimus in mice shows that maximum levels of only 0.1 μM are achieved in a human tumor xenograft following a single administration, whereas plasma levels reach 1 to 3 μM for ~4 h[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
958.22 |
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Formula |
C53H83NO14 |
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CAS 号 |
159351-69-6 |
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中文名称 |
依维莫司 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 54 mg/mL (56.35 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [2] |
Tumor cells are plated into 96-well plates at densities ranging from 500 to 5,000/100 μL/well, with repeat experiments being done at an optimal cell number, typically 1,000 to 2,000 per well, and incubated overnight. Cells are exposed to Everolimus and incubated for 4 days and the cell number is determined by methylene blue staining. For this, 50 μL glutaraldehyde [20% (v/v)] is added to the wells incubated for 10 min at room temperature. The culture medium is aspirated, cells are washed with distilled water, and 100 μL methylene blue [0.05% (w/v) in water] is added and incubated for 10 min at 37°C. Stained cells are washed three times with water, 200 μL HCl [3% (v/v)] is added, and the plate shaken at room temperature for 20 min. The absorbance of each well is determined at 650 nm. The IC50 values are calculated using Softmax 2.0 software[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Mice[2] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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