Everolimus (RAD001)

For research use only. Not for use in humans.

製品コードS1120

Everolimus (RAD001)化学構造

CAS No. 159351-69-6

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 38500 あり
JPY 20200 あり
JPY 36800 あり
JPY 113200 あり
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バルク問合せ

文献中Selleckの製品使用例(587)

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) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
ターゲット
FKBP12 [1]
(Cell-free assay)
mTOR (FKBP12) [1]
(Cell-free assay)
1.6-2.4 nM 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 M4XnW2N6fG:2b4jpZ{BCe3OjeR?= NUSzNXFGPzJiaB?= MX3EUXNQ M4PWe2lEPTB;NT61JO69VQ>? MV6yOFQ1PTNzMR?=
Colo205 Mn3aR5l1d3SxeHnjJGF{e2G7 NXPjdYFZPzJiaB?= M{PXSmROW09? MYnJR|UxRTJyIN88US=> MnjFNlQ1PDV|MUG=
ColoR MmP0R5l1d3SxeHnjJGF{e2G7 M{DKNlczKGh? MXLEUXNQ MnnZTWM2OD16Lkeg{txO NF;YSJIzPDR2NUOxNS=>
HCT116 MVvDfZRwfG:6aXOgRZN{[Xl? M1XLT|czKGh? NFP5W3FFVVOR Mmj6TWM2OD1zMjFOwG0> NXzoO3liOjR2NEWzNVE>
HT29 NYHDOIlLS3m2b4TvfIlkKEG|c3H5 MmTRO|IhcA>? NEXD[GpFVVOR MUDJR|UxRTF3IN88US=> NXi4Wms5OjR2NEWzNVE>
CAKI1 MmT4R5l1d3SxeHnjJGF{e2G7 MYW3NkBp NGS1epVFVVOR NWe1fJp1UUN3ME2xOEDPxE1? MWWyOFQ1PTNzMR?=
SK-HEP1 M1TU[GN6fG:2b4jpZ{BCe3OjeR?= NGCwUXg4OiCq NELa[XZFVVOR NXfJZ5d{UUN3ME2xNkDPxE1? M3zZb|I1PDR3M{Gx
DU145 Mly3R5l1d3SxeHnjJGF{e2G7 MnzMO|IhcA>? M1joWmROW09? MlPyTWM2OD16IN88US=> NILDPGIzPDR2NUOxNS=>
OVCAR3 NXHSeXpmS3m2b4TvfIlkKEG|c3H5 Mn32O|IhcA>? M3G1[mROW09? Ml7iTWM2OD1zNjFOwG0> M1vRWFI1PDR3M{Gx
HOP62 NIfiNoNEgXSxdH;4bYMhSXO|YYm= MXu3NkBp M1vpZ2ROW09? NVviZlgzUUN3ME2xPUDPxE1? NFHEbW4zPDR2NUOxNS=>
Colo205 NGrNT4xHfW6ldHnvckBCe3OjeR?= NYLLOItGOjRiaB?= M2\tRmROW09? Ml;wTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIFPPUG8zODViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHM3KHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hQCC3TR?= Mn7TNlQ5OzZyN{C=
Colo205 M3jxbmZ2dmO2aX;uJGF{e2G7 MYmyOEBp MkjKSG1UVw>? NWfjelNPUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJGNQVE9{MEWgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKDRvRVLQNUBxcG:|cHjvdplt[XSrb36gZZQhOC5zIITvJFghfU1? Mlu3NlQ5OzZyN{C=
SK-HEP1 MUjGeY5kfGmxbjDBd5NigQ>? NHTRUpAzPCCq MlnmSG1UVw>? MmHqTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIGPLMWhGWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHM3KHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hQCC3TR?= M1rlSlI1QDN4MEew
SK-HEP1 NIO0RllHfW6ldHnvckBCe3OjeR?= NH[0WGszPCCq NYK4N2hFTE2VTx?= MUfJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iU1utTGVROSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gOE1GSlBzIIDoc5NxcG:{eXzheIlwdiCjdDCwMlEhfG9iODD1US=> MWmyOFg{PjB5MB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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]
- 合併

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]
- 合併
  • 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]
- 合併
  • 動物モデル: Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.
  • 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 Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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
Storage powder
in solvent
別名 N/A
Smiles CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCO)C)C)O)OC)C)C)C)OC

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02860494 Not yet recruiting Drug: Everolimus|Drug: Placebo Facial Angiofibromas Hospices Civils de Lyon December 2020 Phase 2|Phase 3
NCT04485559 Not yet recruiting Drug: Everolimus|Drug: Trametinib Recurrent World Health Organization (WHO) Grade II Glioma University of California San Francisco|Novartis Pharmaceuticals|Pediatric Brain Tumor Foundation|The Lilabean Foundation for Pediatric Brain Cancer Research August 15 2020 Phase 1
NCT04305444 Recruiting Drug: DTRM-555 Relapsed Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Richter''s Transformation Zhejiang DTRM Biopharma April 24 2020 Phase 2
NCT04258423 Recruiting Drug: Tacrolimus|Drug: Everolimus Kidney Failure Indiana University December 19 2019 Phase 3
NCT03632317 Withdrawn Drug: Panobinostat|Drug: Everolimus Glioma|Diffuse Intrinsic Pontine Glioma University of Michigan Rogel Cancer Center October 2019 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID