Everolimus (RAD001)

For research use only. Not for use in humans.

目录号:S1120 别名: SDZ-RAD 中文名称:依维莫司

Everolimus (RAD001) Chemical Structure

CAS No. 159351-69-6

Everolimus (RAD001, SDZ-RAD)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。Everolimus 可诱导细胞凋亡及自噬并抑制肿瘤细胞的增殖。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1806.72 现货
RMB 898.67 现货
RMB 1731.56 现货
RMB 5477.28 现货
RMB 14062.23 现货
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客户使用Selleck生产的Everolimus (RAD001)发表文献626篇:

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, SDZ-RAD)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。Everolimus 可诱导细胞凋亡及自噬并抑制肿瘤细胞的增殖。
靶点
FKBP12 [1]
(Cell-free assay)
mTOR (FKBP12) [1]
(Cell-free assay)
1.6-2.4 nM 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 Ml\lR5l1d3SxeHnjJGF{e2G7 MVe3NkBp MUHEUXNQ MkLETWM2OD13LkWg{txO NUn5TXNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFU{OTFpPkK0OFQ2OzFzPD;hQi=>
Colo205 M4TPfWN6fG:2b4jpZ{BCe3OjeR?= Mmi0O|IhcA>? M1zIRmROW09? NGSxVlFKSzVyPUKwJO69VQ>? NYTjd3FVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFU{OTFpPkK0OFQ2OzFzPD;hQi=>
ColoR NYC5XnZ5S3m2b4TvfIlkKEG|c3H5 NWjZcWl{PzJiaB?= MXTEUXNQ MVTJR|UxRThwNzFOwG0> NX7jNHMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFU{OTFpPkK0OFQ2OzFzPD;hQi=>
HCT116 NHT2UIdEgXSxdH;4bYMhSXO|YYm= NX7rO29YPzJiaB?= NECxeZlFVVOR NUPPRmVsUUN3ME2xNkDPxE1? MkG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NEWzNVEoRjJ2NES1N|EyRC:jPh?=
HT29 MnGxR5l1d3SxeHnjJGF{e2G7 M3q4RVczKGh? M3XEPGROW09? M4HOdWlEPTB;MUWg{txO MoL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NEWzNVEoRjJ2NES1N|EyRC:jPh?=
CAKI1 NH[zb2REgXSxdH;4bYMhSXO|YYm= MXy3NkBp MonVSG1UVw>? M1LvWmlEPTB;MUSg{txO NH3UR5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0OVMyOSd-MkS0OFU{OTF:L3G+
SK-HEP1 NIXpdHdEgXSxdH;4bYMhSXO|YYm= MknBO|IhcA>? MXrEUXNQ MUXJR|UxRTF{IN88US=> Ml64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NEWzNVEoRjJ2NES1N|EyRC:jPh?=
DU145 MWfDfZRwfG:6aXOgRZN{[Xl? NEfTSII4OiCq M374ZmROW09? MYDJR|UxRThizszN MoW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NEWzNVEoRjJ2NES1N|EyRC:jPh?=
OVCAR3 MkGzR5l1d3SxeHnjJGF{e2G7 NITzSYg4OiCq MYrEUXNQ NEm4doxKSzVyPUG2JO69VQ>? M{LpWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES1N|EyLz5{NES0OVMyOTxxYU6=
HOP62 MnzXR5l1d3SxeHnjJGF{e2G7 M{HqZVczKGh? NH;SfFhFVVOR Mm\ZTWM2OD1zOTFOwG0> NV3GOnBGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFU{OTFpPkK0OFQ2OzFzPD;hQi=>
Colo205 M1fie2Z2dmO2aX;uJGF{e2G7 M37tXlI1KGh? MYnEUXNQ M33NVGlvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDDU2xQOjB3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBUPiCyaH;zdIhwenmuYYTpc44h[XRiMD6xJJRwKDhidV2= NYj1VllCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4N|YxPzBpPkK0PFM3ODdyPD;hQi=>
Colo205 M4rXPWZ2dmO2aX;uJGF{e2G7 NYHWd3BxOjRiaB?= NW\qdXFRTE2VTx?= NF7ab5JKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gR29NVzJyNTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhPC2HQmCxJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gPEB2VQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh|NkC3NEc,OjR6M{[wO|A9N2F-
SK-HEP1 NGHZcJpHfW6ldHnvckBCe3OjeR?= MWSyOEBp NH7nfmVFVVOR MYjJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iU1utTGVROSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KDBwMTD0c{A5KHWP NUG0N|FWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4N|YxPzBpPkK0PFM3ODdyPD;hQi=>
SK-HEP1 M4juPWZ2dmO2aX;uJGF{e2G7 MnP0NlQhcA>? NYH5b3RRTE2VTx?= NFrNNGNKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gV2suUEWSMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhPC2HQmCxJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gPEB2VQ>? M2\INFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEO2NFcxLz5{NEizOlA4ODxxYU6=
Sf9 NFPrcopHfW6ldHnvckBCe3OjeR?= MVGxOUB1dyB{MDDtbY5{ NUe4ZZY6UW6qaXLpeIlwdiCxZjDoeY1idiCEU1XQJI93\XKneIDy[ZN{\WRiaX6gV4Y6KGOnbHygcYVu[nKjbnWgeoV{cWOuZYOgZZN{\XO|ZXSgZZMhfXC2YXvlJI9nKFt|SG2teIF2em:laH;sZZRmKGmwIIDy[ZNmdmOnIH;mJGFVWCCvZXHzeZJm\CCjZoTldkAyPSC2bzCyNEBucW6|IHL5JI1mdWK{YX7lJJZme2mlbHWgeJJidnOyb4L0JIF{e2G7LDDJR|UxKD1iMjFOwG0v Mln1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NU[xNFEoRjJ|OUW2NVAyRC:jPh?=
Sf9 MXfGeY5kfGmxbjDBd5NigQ>? M17xTVIxKG2rboO= MoDmTY5pcWKrdHnvckBw\iCqdX3hckBOWlB{IH;2[ZJmgHC{ZYPz[YQhcW5iU3[5JINmdGxibXXtZpJidmVidnXzbYNt\XNiYYPz[ZN{\WRiYYOgeZB1[WunIH;mJHs{UF1vZYP0doFlcW:uLUG3ZoV1[S2GLXfseYN2em:waXTlJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmRiR2PIJI1m[XO3cnXkJIFnfGW{IEKwJI1qdnNiYomgcYVu[nKjbnWgeoV{cWOuZTD0doFve3CxcoSgZZN{[XluIFnDOVAhRSBzMT6zJO69VS5? MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NU[xNFEoRjJ|OUW2NVAyRC:jPh?=
A549 M{\4O2F2fG:yaHHnfUBie3OjeR?= NVTobno1PSC3TR?= MXS2JIg> MnvjTY5lfWO2aX;uJI9nKGG3dH;wbIFogSCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOxbo\ldpNqd25ib3[gUGM{NTFidH:gUGM{NTJiYYSgOUB2VSCjZoTldkA3KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MmDGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzN{[xOlUoRjJ4MUe2NVY2RC:jPh?=
A549 MXXGeY5kfGmxbjDBd5NigQ>? NEHHR442KHWP NYHue2F4OyC2bzCyOEBp MVnJcohq[mm2aX;uJI9nKG2WT2KgdIhwe3Cqb4L5cIF1cW:wIHH0JJNmejJ2NEigbY4hcHWvYX6gRVU1QSClZXzsd{BifCB3IIXNJIFnfGW{IEOgeI8hOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M2\PWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUe2NVY2Lz5{NkG3OlE3PTxxYU6=
A549 MWrGeY5kfGmxbjDBd5NigQ>? NEH2bY02KHWP MkGyN{B1dyB{NDDo MUTJcohq[mm2aX;uJI9nKG2WT2KgbY4hcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCyN{DTOmsheGixc4Doc5J6dGG2aX;uJIF1KHSqckO4PUBifCB3IIXNJIFnfGW{IEOgeI8hOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M{XkVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUe2NVY2Lz5{NkG3OlE3PTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Mcl-1 / p-ERK / S6K1(T389); 

PubMed: 27351224     


Ten CRC cell lines with BRAF WT or 600E were treated with Everolimus for 24 h and analyzed by western blotting.

pS6RP; 

PubMed: 25014496     


Western blots showing the phosphorylation of S6RP in NALM6 cells following treatment with indicated concentrations of everolimus over various time intervals.

cleaved caspase-3 ; 

PubMed: 27351224     


Cells treated with 20 μM Everolimus for 24 h were analyzed by western blotting

27351224 25014496
Growth inhibition assay
Cell counts; 

PubMed: 27127803     


Primary human coronary artery vascular smooth muscle cells (hSMC) were serum-deprived (−) and treated with vehicle or the indicated doses of everolimus in growth medium. Cell counts are expressed as mean ± SEM (n = 12 samples/group) relative to quiescent hSMC.

IC50; 

PubMed: 23509629     


Average IC50 values of everolimus in HCC cell lines. Cumulative results from 3 independent experiments were shown as mean ± SEM. 

Cell proliferation; 

PubMed: 21135857     


Dose-dependent inhibition of mantle cell proliferation (Jeko) and diffuse large B-cell lymphoma cell proliferation (DHL6) with the mTOR inhibitor everolimus. 

27127803 23509629 21135857
Immunofluorescence
TERT; 

PubMed: 27127803     


Immunostaining for TERT expression (green) in WT mSMC treated with 10 μmol/l everolimus. 4′-6-diamidino-2-phenylindole (DAPI) was used for nuclear staining. Images are representative of 3 independently performed experiments.

27127803
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]
- 合并

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]
- 合并
  • 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]
- 合并
  • Animal Models: 在左乳房垫下方注射培养的BT474干细胞的BALB/ C裸鼠
  • 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)
Water Insoluble
Ethanol '7 mg/mL
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
储存条件 粉状
溶于溶剂
别名 SDZ-RAD

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02155920 Active not recruiting Drug: Everolimus Recurrent Childhood Ependymoma University of Texas Southwestern Medical Center February 2015 Phase 2
NCT01997255 Withdrawn Drug: Everolimus Sturge Weber Syndrome Baylor College of Medicine|Novartis Pharmaceuticals April 2014 Phase 2
NCT02305810 Completed Drug: Everolimus 10 mg daily Pancreatic Neuroendocrine Tumour Metastatic European Institute of Oncology September 2013 Phase 2
NCT01939418 Terminated Drug: RAD001|Drug: Gemcitabine|Drug: Cisplatin Metastatic Breast Cancer National Cancer Center Korea August 2013 Phase 1|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.

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