Everolimus (RAD001)

目录号:S1120

Everolimus (RAD001) Chemical Structure

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。

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客户购买Selleck的此次产品后发表的文献50篇:

客户使用该产品的6个实验数据:

  • 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.

  • 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.

    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.

    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。
靶点
mTOR (FKBP12) [1]
(Cell-free assay)
1.6 nM-2.4 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SQ20B M4\SXmN6fG:2b4jpZ{BCe3OjeR?= NHjxSmY4OiCq NXXlUYVtTE2VTx?= MkHkTWM2OD13LkWg{txO NYD4eZJvOjR2NEWzNVE>
Colo205 M4\jO2N6fG:2b4jpZ{BCe3OjeR?= MYS3NkBp MmXnSG1UVw>? MmLkTWM2OD1{MDFOwG0> NHzGRlkzPDR2NUOxNS=>
ColoR NF[4O4REgXSxdH;4bYMhSXO|YYm= MUm3NkBp NWjUXJNSTE2VTx?= MYHJR|UxRThwNzFOwG0> NYDqXWhGOjR2NEWzNVE>
HCT116 NXHkb2dLS3m2b4TvfIlkKEG|c3H5 MUe3NkBp M3P1XGROW09? M1T6W2lEPTB;MUKg{txO M4D2[VI1PDR3M{Gx
HT29 Mn\PR5l1d3SxeHnjJGF{e2G7 MnTwO|IhcA>? MUXEUXNQ MXTJR|UxRTF3IN88US=> MV:yOFQ1PTNzMR?=
CAKI1 NH;ySlhEgXSxdH;4bYMhSXO|YYm= MV[3NkBp MnLuSG1UVw>? NUPKS3ZPUUN3ME2xOEDPxE1? MXSyOFQ1PTNzMR?=
SK-HEP1 MVPDfZRwfG:6aXOgRZN{[Xl? M{O4RVczKGh? NWH1RnR6TE2VTx?= MXnJR|UxRTF{IN88US=> NWP4enltOjR2NEWzNVE>
DU145 MljmR5l1d3SxeHnjJGF{e2G7 MU[3NkBp Mm\0SG1UVw>? M{PZdWlEPTB;ODFOwG0> NFHmUVkzPDR2NUOxNS=>
OVCAR3 M173R2N6fG:2b4jpZ{BCe3OjeR?= MnTEO|IhcA>? M1S1c2ROW09? MXrJR|UxRTF4IN88US=> NWfGcXNjOjR2NEWzNVE>
HOP62 NHe5bm5EgXSxdH;4bYMhSXO|YYm= M4PVRlczKGh? NITmcmdFVVOR NX3XTlVxUUN3ME2xPUDPxE1? M4nle|I1PDR3M{Gx
Colo205 M4K3[2Z2dmO2aX;uJGF{e2G7 NVvRRXJIOjRiaB?= NEDJe|RFVVOR NWHUdXpGUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJGNQVE9{MEWgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKFN4IIDoc5NxcG:{eXzheIlwdiCjdDCwMlEhfG9iODD1US=> NVHDW2w3OjR6M{[wO|A>
Colo205 NFHKcpZHfW6ldHnvckBCe3OjeR?= Mn6yNlQhcA>? Mn\ISG1UVw>? NHj2WGpKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gR29NVzJyNTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhPC2HQmCxJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gPEB2VQ>? MY[yOFg{PjB5MB?=
SK-HEP1 Mme1SpVv[3Srb36gRZN{[Xl? NU\sNHdjOjRiaB?= M{TXb2ROW09? M3vyS2lvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDTT{1JTVBzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBUPiCyaH;zdIhwenmuYYTpc44h[XRiMD6xJJRwKDhidV2= M1XBTFI1QDN4MEew
SK-HEP1 M1Ttc2Z2dmO2aX;uJGF{e2G7 M1\vfVI1KGh? Ml64SG1UVw>? Mn\yTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIGPLMWhGWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJFQuTUKSMTDwbI9{eGixconsZZRqd25iYYSgNE4yKHSxIEigeW0> MlP6NlQ5OzZyN{C=

... Click to View More Cell Line Experimental Data

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]
+ 展开

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)。
细胞实验:[3]
+ 展开
  • Cell lines: BT474细胞系和原发性乳腺癌细胞
  • Concentrations: 0.001 μM 到10 μM
  • Incubation Time: 24小时
  • Method: 通过MTT 实验比较Everolimus 或Trastuzumab作用于全部乳腺癌细胞和乳腺CSCs的效果。BT474 细胞系和原发性乳腺癌细胞的全部细胞和干细胞分别接种在含不同浓度药物的96孔板中,每种浓度重复放置5个孔,然后细胞在37oC下温育24小时。Everolimus 浓度为1 nM, 10 nM, 100 nM, 1 μM 和 10 μM, Trastuzumab 浓度为 0.5 μg/mL, 1 μg/mL, 10 μg/mL, 50 μg/mL,和 100 μg/mL。通过MTT实验,使用 10 μg/mL Trastuzumab和浓度不断增高的Everolimus (1 nM, 10 nM, 100 nM 和1 μM),测定Everolimus 和Trastuzumab 联用,在体外作用于乳腺 CSCs 生长的效果。药物处理24小时后, 每孔加入溶于PBS的20 μL 5 mg/mL MTT, 然后细胞在37oC下在含5 % CO2 及饱和湿度环境下温育4小时。随后除去上清液, 每孔加入150 μL DMSO,细胞涡旋10分钟。使用ELISA读数器测定每孔的吸光值(OD值)。每组实验重复进行三次,绘制剂量反应曲线。使用用于Windows的概率统计软件包SPSS17.0软件计算IC50值。
    (Only for Reference)
动物实验:[3]
+ 展开
  • Animal Models: 在左乳房垫下方注射培养的BT474干细胞的BALB/ C裸鼠
  • Formulation: 溶于盐水中
  • Dosages: ≤2 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (104.36 mM)
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
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

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

  • 质量
    浓度
    体积
    分子量

*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

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 )

  • C1
    V1
    C2
    V2

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。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01231659 Completed Postmenopausal Women|Locally Advanced Metastatic Breast Cancer|Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis August 9 2011 Phase 4
NCT03114527 Recruiting Soft Tissue Sarcoma Fox Chase Cancer Center August 8 2017 Phase 2
NCT02315625 Recruiting Neuroendocrine Tumors|Neuroendocrine Carcinoma|Neuroendocrine Neoplasms|Carcinoma Neuroendocrine|Neuroendocrine Tumors of the Gastrointestinal Tract and Pancreas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 8 2015 Phase 2
NCT01529554 Recruiting Acute Coronary Syndromes University of Zurich|Swiss National Science Foundation|Novartis January 8 2015 Phase 1|Phase 2
NCT02015559 Active not recruiting Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Oral Complications|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI) October 8 2014 Phase 2
NCT01567488 Completed Gastrointestinal Neoplasms Grupo Espanol de Tumores Neuroendocrinos June 8 2011 Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 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?

  • 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.

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID