Everolimus (RAD001)

製品コードS1120

Everolimus (RAD001)化学構造

分子量(MW):958.22

Everolimus (RAD001)は一種のmTOR阻害剤で、FKBP12に作用します。無細胞試験でIC50値は1.6-2.4 nMになります。

サイズ 価格 在庫  
USD 277 あり
USD 138 あり
USD 264 あり
USD 844 あり

文献中の引用(50)

カスタマーフィードバック(6)

  • 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.

    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 . 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.

    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.

  • 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.

製品安全説明書

mTOR阻害剤の選択性比較

生物活性

製品説明 Everolimus (RAD001)は一種のmTOR阻害剤で、FKBP12に作用します。無細胞試験でIC50値は1.6-2.4 nMになります。
ターゲット
mTOR (FKBP12) [1]
(Cell-free assay)
1.6 nM-2.4 nM
体外試験

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. [1] Everolimus also shows antiangiogenic/vascular effects in VEGF-induced HUVEC proliferation with IC50 of 0.12 nM and bFGF-induced HUVEC proliferation with IC50 of 0.8 nM, respectively. [2] A recent study shows that Everolimus shows a dose-dependent inhibitory effects on both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells with IC50 of 156 nM in total cells of primary breast cancer cells and 71 nM in total cells of BT474 cells. In addition, combination treatment with Everolimus and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SQ20B NYXodVFHS3m2b4TvfIlkKEG|c3H5 MUK3NkBp MX;EUXNQ MXfJR|UxRTVwNTFOwG0> NW\TUIduOjR2NEWzNVE>
Colo205 NGL5[nREgXSxdH;4bYMhSXO|YYm= MVW3NkBp MVrEUXNQ NVvVNZlZUUN3ME2yNEDPxE1? NXfDPZd4OjR2NEWzNVE>
ColoR M{\6XmN6fG:2b4jpZ{BCe3OjeR?= MWS3NkBp NVzXVm9VTE2VTx?= MXrJR|UxRThwNzFOwG0> M13BO|I1PDR3M{Gx
HCT116 MlXUR5l1d3SxeHnjJGF{e2G7 NEDSZXU4OiCq MWHEUXNQ NUnUcWFuUUN3ME2xNkDPxE1? M2fXeFI1PDR3M{Gx
HT29 NI\4eYJEgXSxdH;4bYMhSXO|YYm= NHe2UWs4OiCq Mn\4SG1UVw>? M17LUWlEPTB;MUWg{txO NVvvbYRxOjR2NEWzNVE>
CAKI1 Ml[2R5l1d3SxeHnjJGF{e2G7 NX;VOmk5PzJiaB?= M{e1UWROW09? MW\JR|UxRTF2IN88US=> MXOyOFQ1PTNzMR?=
SK-HEP1 M3OyW2N6fG:2b4jpZ{BCe3OjeR?= M1TkPVczKGh? MoLySG1UVw>? MYXJR|UxRTF{IN88US=> MYqyOFQ1PTNzMR?=
DU145 NIHRcoFEgXSxdH;4bYMhSXO|YYm= NInyTnI4OiCq NXvqW5BiTE2VTx?= NGPpOYdKSzVyPUig{txO M2nWOFI1PDR3M{Gx
OVCAR3 NUHuUmIyS3m2b4TvfIlkKEG|c3H5 M4C3S|czKGh? NG\PXHNFVVOR MoLITWM2OD1zNjFOwG0> M2L5[|I1PDR3M{Gx
HOP62 NYG2cWt{S3m2b4TvfIlkKEG|c3H5 NH71Tmk4OiCq NHziXpNFVVOR MmCwTWM2OD1zOTFOwG0> MUWyOFQ1PTNzMR?=
Colo205 NXTQeplOTnWwY4Tpc44hSXO|YYm= NWTxN2hYOjRiaB?= NXu1TW5MTE2VTx?= MXHJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KDBwMTD0c{A5KHWP MVeyOFg{PjB5MB?=
Colo205 M2C5TWZ2dmO2aX;uJGF{e2G7 NWSx[4xnOjRiaB?= NXnC[WNRTE2VTx?= M1yyPWlvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDDU2xQOjB3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kA1NUWEUEGgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC2bzC4JJVO MVGyOFg{PjB5MB?=
SK-HEP1 Mle2SpVv[3Srb36gRZN{[Xl? MoCwNlQhcA>? NH;JT2pFVVOR NHLucJVKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gV2suUEWSMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhWzZicHjvd5Bpd3K7bHH0bY9vKGG2IECuNUB1dyB6IIXN M1n0ZlI1QDN4MEew
SK-HEP1 Mnu1SpVv[3Srb36gRZN{[Xl? NYjkXXpsOjRiaB?= NVrCRoExTE2VTx?= NGDhRnpKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gV2suUEWSMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhPC2HQmCxJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gPEB2VQ>? NXPTeoRbOjR6M{[wO|A>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Everolimus (0.1 to 10 mg/kg) dose-dependently inhibits growth of the primary (ear) and lymph node metastases of B16/BL6 melanoma, with decreased total number of vessels and reduced mature vessels. [2] In a xenograft animal model of BT474 stem cells, Everolimus shows significant reductions in mean tumor sizes (590.6 mm3), compared to the control group with a tumor size of 698 mm3. Furthermore, combination treatment with Everolimus and trastuzumab significantly decreases the xenograft tumor size (410.8 mm3) more than Everolimus treatment alone. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

FKBP12 binding assay & Mixed lymphocyte reaction (MLR) :

FKBP12 binding assay: Binding to the FK 506 binding protein (FKBP12) is indirectly assessed by means of an ELISA-type competition assay. FK 506 is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to FK 506 (rIC50 = IC50 Everolimus/IC50 FK 506). Mixed lymphocyte reaction (MLR): The immunosuppressive activities of RAP and its derivatives are assessed in a two-way MLR, using spleen cells of BALB/c and CBA mice. RAP is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to RAP (rIC50 = IC50 Everolimus/IC50 RAP).
細胞試験: [3]
+ 展開
  • 細胞株: BT474 cell line and the primary breast cancer cells
  • 濃度: 0.001-10 μM
  • 反応時間: 24 hours
  • 実験の流れ: The 3-(4-5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction assay (MTT assay) is used to compare the effects of Everolimus or trastuzumab on total breast cancer cells and breast CSCs. The total cells and the stem cells from the BT474 cell line and the primary breast cancer cells are respectively seeded into 96-well plates with different concentrations of the drugs, with five wells for each concentration, and the cells are cultured at 37 °C with 5 % CO2 in an incubator for 24 hours. The concentrations of Everolimus are 1 nM, 10 nM, 100 nM, 1 μM and 10 μM, and the concentrations of trastuzumab are 0.5 μg/mL, 1 μg/mL, 10 μg/mL, 50 μg/mL, and 100 μg/mL. The combinatorial inhibitory effect of Everolimus and Trastuzumab on the in vitro growth of breast CSCs is examined by MTT assay as well using 10 μg/mL trastuzumab in combination of increasing concentrations of everolimus (1 nM, 10 nM, 100 nM and 1 μM). After drug treatment for 24 hours, 20 μL MTT [5 mg/mL in phosphate buffered saline (PBS)] is added to each well, and the cells are incubated at 37 °C with 5 % CO2 and saturated humidity for 4 hours. Following the subsequent removal of the supernatant, 150 μL dimethyl sulfoxide (DMSO) is added to each well, and the cells are vortexed for 10 minutes. The light absorbance (OD value) is measured for each well using an ELISA reader. Each experiment is repeated in triplicate, and dose–response curves are plotted. The probit software of the statistical software package SPSS 17.0 for Windows is used to calculate the inhibitory concentration (IC50) of Everolimus.
    (参考用のみ)
動物試験:[3]
+ 展開
  • 動物モデル: Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.
  • 製剤: Everolimus is dissolved in saline.
  • 投薬量: ≤2 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (104.36 mM)
Ethanol 7 mg/mL (7.3 mM)
Water slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 958.22
化学式

C53H83NO14

CAS No. 159351-69-6
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02352844 Recruiting Solid Malignancy|Solid Tumor Washington University School of Medicine October 7, 2015 Phase 2
NCT02315625 Recruiting Neuroendocrine Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 5, 2014 Phase 2
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5, 2013 Phase 1|Phase 2
NCT01797120 Active, not recruiting Metastatic Breast Cancer PrECOG, LLC.|Novartis May 31, 2013 Phase 2
NCT01784861 Recruiting Adenocarcinoma|Pancreatic Neoplasms Washington University School of Medicine May 3, 2013 Phase 1|Phase 2
NCT02890069 Recruiting Colorectal Cancer|Non-small Cell Lung Carcinoma (Adenocarcinoma)|Triple Negative Breast Cancer Novartis Pharmaceuticals|Novartis October 26, 2016 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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信号経路図

mTOR Inhibitors with Unique Features

相関mTOR製品

Tags: Everolimus (RAD001)を買う | Everolimus (RAD001) ic50 | Everolimus (RAD001)供給者 | Everolimus (RAD001)を購入する | Everolimus (RAD001)費用 | Everolimus (RAD001)生産者 | オーダーEverolimus (RAD001) | Everolimus (RAD001)化学構造 | Everolimus (RAD001)分子量 | Everolimus (RAD001)代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID