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
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客户使用Selleck生产的Everolimus (RAD001)发表文献658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 MmraR5l1d3SxeHnjJGF{e2G7 MXm3NkBp M{TDdGROW09? Mkf2TWM2OD13LkWg{txO NY\TRmt4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFU{OTFpPkK0OFQ2OzFzPD;hQi=>
Colo205 MX\DfZRwfG:6aXOgRZN{[Xl? NVzLPY1wPzJiaB?= NEHkXHVFVVOR NEG5PHpKSzVyPUKwJO69VQ>? NGrTWVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0OVMyOSd-MkS0OFU{OTF:L3G+
ColoR MoO1R5l1d3SxeHnjJGF{e2G7 NEHlVoY4OiCq MnfTSG1UVw>? MV7JR|UxRThwNzFOwG0> M4\JbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES1N|EyLz5{NES0OVMyOTxxYU6=
HCT116 MlnIR5l1d3SxeHnjJGF{e2G7 MXy3NkBp MXLEUXNQ M{j1bmlEPTB;MUKg{txO M4\IXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES1N|EyLz5{NES0OVMyOTxxYU6=
HT29 MljNR5l1d3SxeHnjJGF{e2G7 NUDFfXRGPzJiaB?= MXTEUXNQ MmLZTWM2OD1zNTFOwG0> M3LhSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES1N|EyLz5{NES0OVMyOTxxYU6=
CAKI1 NIL3e3JEgXSxdH;4bYMhSXO|YYm= MnPRO|IhcA>? NWnOVoJ1TE2VTx?= MnjJTWM2OD1zNDFOwG0> NFXDT3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0OVMyOSd-MkS0OFU{OTF:L3G+
SK-HEP1 M{HabGN6fG:2b4jpZ{BCe3OjeR?= NEKwW4Q4OiCq M1rJ[GROW09? MWnJR|UxRTF{IN88US=> NF;RZ4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0OVMyOSd-MkS0OFU{OTF:L3G+
DU145 M3T2RWN6fG:2b4jpZ{BCe3OjeR?= Ml3pO|IhcA>? MXvEUXNQ MX7JR|UxRThizszN NETSdWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0OVMyOSd-MkS0OFU{OTF:L3G+
OVCAR3 M1K2NmN6fG:2b4jpZ{BCe3OjeR?= M3P2dFczKGh? NFf5cHZFVVOR M13vcmlEPTB;MU[g{txO MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR2NUOxNUc,OjR2NEWzNVE9N2F-
HOP62 NYnON|U{S3m2b4TvfIlkKEG|c3H5 MXK3NkBp M{npe2ROW09? NX\6TJRjUUN3ME2xPUDPxE1? M1zrbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES1N|EyLz5{NES0OVMyOTxxYU6=
Colo205 M3;VU2Z2dmO2aX;uJGF{e2G7 Ml3MNlQhcA>? MWDEUXNQ NW\X[XRsUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJGNQVE9{MEWgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKFN4IIDoc5NxcG:{eXzheIlwdiCjdDCwMlEhfG9iODD1US=> NIfVT489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEizOlA4OCd-MkS4N|YxPzB:L3G+
Colo205 MWfGeY5kfGmxbjDBd5NigQ>? MnnONlQhcA>? NInaTIlFVVOR NVfjW|JlUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJGNQVE9{MEWgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKDRvRVLQNUBxcG:|cHjvdplt[XSrb36gZZQhOC5zIITvJFghfU1? MlTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6M{[wO|AoRjJ2OEO2NFcxRC:jPh?=
SK-HEP1 M2LNZ2Z2dmO2aX;uJGF{e2G7 NXLnTpRzOjRiaB?= NY\DN49QTE2VTx?= M{C2eWlvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDTT{1JTVBzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBUPiCyaH;zdIhwenmuYYTpc44h[XRiMD6xJJRwKDhidV2= NFT3Xmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEizOlA4OCd-MkS4N|YxPzB:L3G+
SK-HEP1 MnfXSpVv[3Srb36gRZN{[Xl? M{HieVI1KGh? NYnjXVBrTE2VTx?= NXLpN3RUUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJHNMNUiHUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKDRvRVLQNUBxcG:|cHjvdplt[XSrb36gZZQhOC5zIITvJFghfU1? MmjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6M{[wO|AoRjJ2OEO2NFcxRC:jPh?=
Sf9 NYTYNGVXTnWwY4Tpc44hSXO|YYm= M13uOVE2KHSxIEKwJI1qdnN? NWi0cmtqUW6qaXLpeIlwdiCxZjDoeY1idiCEU1XQJI93\XKneIDy[ZN{\WRiaX6gV4Y6KGOnbHygcYVu[nKjbnWgeoV{cWOuZYOgZZN{\XO|ZXSgZZMhfXC2YXvlJI9nKFt|SG2teIF2em:laH;sZZRmKGmwIIDy[ZNmdmOnIH;mJGFVWCCvZXHzeZJm\CCjZoTldkAyPSC2bzCyNEBucW6|IHL5JI1mdWK{YX7lJJZme2mlbHWgeJJidnOyb4L0JIF{e2G7LDDJR|UxKD1iMjFOwG0v M1XvTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW2NVAyLz5{M{m1OlExOTxxYU6=
Sf9 NWjm[YhWTnWwY4Tpc44hSXO|YYm= Ml7INlAhdWmwcx?= M2PteWlvcGmkaYTpc44hd2ZiaIXtZY4hVVKSMjDveoVz\XiycnXzd4VlKGmwIGPmPUBk\WyuIH3lcYJz[W6nII\ld4lkdGW|IHHzd4V{e2WmIHHzJJVxfGGtZTDv[kBcO0ifLXXzeJJi\GmxbD2xO4JmfGFvRD3ncJVkfXKxbnnk[UBqdiCycnXz[Y5k\SCxZjDBWHAh[W6mIFfTTEBu\WG|dYLl[EBi\nSncjCyNEBucW6|IHL5JI1mdWK{YX7lJJZme2mlbHWgeJJidnOyb4L0JIF{e2G7LDDJR|UxKD1iMUGuN{DPxE1w MmTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NU[xNFEoRjJ|OUW2NVAyRC:jPh?=
A549 NIP1UZdCfXSxcHjh[5kh[XO|YYm= NYTGXldqPSC3TR?= NIq4eoU3KGh? NVjZZmhsUW6mdXP0bY9vKG:oIHH1eI9xcGGpeTDpckBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPvcpZmenOrb36gc4YhVEN|LUGgeI8hVEN|LUKgZZQhPSC3TTDh[pRmeiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NHvIT4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG3OlE3PSd-Mk[xO|YyPjV:L3G+
A549 M1W2VGZ2dmO2aX;uJGF{e2G7 NHzUZ242KHWP NIi5XYI{KHSxIEK0JIg> NIDQUmZKdmirYnn0bY9vKG:oIH3UU3IheGixc4Doc5J6dGG2aX;uJIF1KHOnckK0OFghcW5iaIXtZY4hSTV2OTDj[YxteyCjdDC1JJVOKGGodHXyJFMhfG9iMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NFnWbYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG3OlE3PSd-Mk[xO|YyPjV:L3G+
A549 MkLQSpVv[3Srb36gRZN{[Xl? MYO1JJVO MknWN{B1dyB{NDDo MlLZTY5pcWKrdHnvckBw\iCvVF;SJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZicEewV|ZMKHCqb4PwbI9zgWyjdHnvckBifCC2aIKzPFkh[XRiNTD1UUBi\nSncjCzJJRwKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NXn0dZVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xO|YyPjVpPkK2NVc3OTZ3PD;hQi=>

... 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
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