Everolimus (RAD001)
目录号：S1120
Molecular Weight(MW): 958.22
Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。
客户使用该产品的7个实验数据：
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Effects on PI3K signaling. Tumor cells were treated with DMSO, BEZ-235 (5uM, 1uM), BKM-120 (5uM, 1uM), RAD-001(5uM, 1uM) or cyclopamine (2.5uM, 1uM) for 3 hr. Cells were lysed and protein was analyzed for phosphorylation of AKT and S6 (pAKT and pS6) or for GAPDH by Western blotting.
Cancer Cell 2012 21(2), 155-67. Everolimus (RAD001) purchased from Selleck.
Treatment of the BRAFi-resistant melanoma cells with the mTOR inhibitor RAD001 did lead to substantial decrease of S6 phosphorylation in the 3 BRAFi-resistant lines K028PR, M34PR, and K029PR; however, such an inhibition failed to elicit any inhibitory effect on the expression of PD-L1.
Clin Cancer Res 2013 19(3),598-609. Everolimus (RAD001) purchased from Selleck.
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Effects of RAD001 on the phosphorylation levels of key components of the PI3K/Akt/mTOR pathway after 4 h of treatment with increasing concentrations of the drug. (a) Western blot analysis for mTOR and its downstream targets, p70S6K and 4EBP1. (b) Western blot analysis for Akt, GSK3-α/β and FoxO3A. In a and b, 50 μg of protein was blotted to each lane. β-actin served as a loading control.
Leukemia, 2014, 28(4):739-48. Everolimus (RAD001) purchased from Selleck.
C) Knockdown of AURKA in RAD001 resistant FLO-1 or SK-GT-4 cells downregulated p-EIF4E (S209) and c-MYC proteins, with or without RAD001 treatment. D) Pharmacological inhibition of AURKA using alisertib led to downregulation of p-EIF4E (S209) and c-MYC proteins in FLO-1 and SK-GT-4 resistant cells, with or without RAD001 treatment
Clin Cancer Res, 2017, 23(14):3756-3768. Everolimus (RAD001) purchased from Selleck.
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Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
Br J Cancer 2014 111(6), 1168-79. Everolimus (RAD001) purchased from Selleck.
The phenotype of nuclear blebbing was improved in RAD001 and rapamycin treated HGPS fibroblast cells. Cells were stained with DAPI (blue), laminA/C antibody (red), and progerin antibody (green) to show nuclear location and morphology. The treatment duration is for seven weeks. Mock: vehicle (DMSO, 0.025% v/v); Rap: 0.68 uM rapamycin, Rad: 0.1 uM RAD001. (Scale bar: 10 um)
Aging (Albany NY) 2012 4(2), 119-32. Everolimus (RAD001) purchased from Selleck.
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Inhibition of mTOR activity may be responsible for sorafenib-induced down-regulation of survivin. H1299 cells were treated with the indicated concentration of RAD001 or Rapamycin for 48 h. Then H1299 cells were incubated with or without 5 μM sorafenib, with or without 5 μM RAD001, and with or without 2 μM rapamycin for 48 h. The indicated protein levels were determined by Western blot analysis. b-Actin protein levels were measured as loading controls.
Biochem Pharmacol 2011 82, 216-226. Everolimus (RAD001) purchased from Selleck.
产品安全说明书
mTOR抑制剂选择性比较
生物活性
| 产品描述 | Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 体外研究 |
体外, 与Rapamycin相比，Everolimus 具有抑制免疫活性。Everolimus与固定化的FK 506竞争性结合到生物素化的FKBP12上，IC50为1.6 nM-2.4 nM,且作用于BALB/c和CBA小鼠脾脏细胞，抑制双向MLR，IC50为0.12 nM-1.8 nM。[1]Everolimus 作用于VEGF诱导的HUVEC增殖和bFGF诱导的 HUVEC增殖，具有抗血管生成/血管效果，IC50分别为0.12 nM和 0.8 nM。[2]最新研究显示Everolimus抑制BT474 细胞系和原发性乳腺癌细胞的全部细胞和干细胞，作用于原发性乳腺癌的全部细胞时IC50为 156 nM，作用于BT474细胞的全部细胞时，IC50为71 nM。此外, Everolimus和Trastuzumab联用，显著促进对肿瘤干细胞生长的抑制作用，抑制率提高50%以上。 [3] |
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| Cell Data |
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| 体内研究 | Everolimus (0.1 到 10 mg/kg)抑制B16/BL6黑色素瘤的原代生长和淋巴结转移，伴随着全部血管数降低，这种作用存在剂量依赖性。[2] Everolimus作用于携带BT474干细胞移植瘤动物模型，与对照组相比（体积为698 mm3），显著降低平均肿瘤尺寸(590.6 mm3)。而且,与 Everolimus单独处理相比，Everolimus和Trastuzumab联用显著降低移植瘤尺寸 (410.8 mm3)。[3] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验：[1] |
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FKBP12结合试验及混合淋巴细胞反应（MLR）: FKBP12 结合实验：通过 ELISA-型竞争性检测法直接测量与FK 506 结合蛋白(FKBP12)的结合情况。每组实验中的FK 506作为标准与FK 506相比，抑制活性表示为相对IC50值。(rIC50 = IC50 Everolimus /IC50 FK 506)。混合淋巴细胞反应 (MLR): 在双向MLR中，使用BALB/c和CBA小鼠脾细胞，测量RAP及其衍生物的抑制免疫反应活性。每组实验中RAP作为标准，与RAP相比，抑制活性表示为相对IC50值(rIC50 = IC50 Everolimus /IC50 RAP)。 |
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| 细胞实验：[3] |
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| 动物实验：[3] |
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溶解度 (25°C)
| 体外 | DMSO | 100 mg/mL (104.36 mM) |
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| Ethanol | 7 mg/mL (7.3 mM) | |
| Water | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 958.22 |
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| 化学式 | C53H83NO14 |
| CAS号 | 159351-69-6 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03324373 | Not yet recruiting | Renal Cell Carcinoma | Yousef Zakharia|Eisai Research Institute|University of Iowa | April 30 2019 | Phase 1 |
| NCT03454724 | Not yet recruiting | Coronary Artery Disease | Meril Life Sciences Pvt. Ltd. | April 1 2019 | Not Applicable |
| NCT03454724 | Not yet recruiting | Coronary Artery Disease | Meril Life Sciences Pvt. Ltd. | April 1 2019 | Not Applicable |
| NCT03324373 | Not yet recruiting | Renal Cell Carcinoma | Yousef Zakharia|Eisai Research Institute|University of Iowa | April 30 2019 | Phase 1 |
| NCT03654040 | Not yet recruiting | Liver Transplant | National Institute of Allergy and Infectious Diseases (NIAID)|Immune Tolerance Network (ITN) | March 2019 | Phase 1|Phase 2 |
| NCT03878524 | Not yet recruiting | Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia | OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation | March 14 2019 | Phase 1 |
技术支持
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如果有其他问题，请给我们留言。
常见问题及建议解决方法
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问题 1：
For the in vivo work, I know the drug needs to be dissolved in 30% propylene glycol (dilution in water) and 5%Tween 80. Would the final solution be a clear liquid or a turbid suspension?
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回答：
Our S1120 Everolimus (RAD001) in 30% Propylene glycol+5% Tween 80+ddH2O at 5mg/ml is a clear solution. And for oral gavage, there is another common vehicle, 1% CMC Na. Everolimus can be dissolved in it at 30mg/ml as a suspension.
