Everolimus

別名:RAD001,SDZ-RAD

エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。

Everolimus化学構造

CAS No. 159351-69-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 33000 国内在庫あり
JPY 22000 国内在庫あり
JPY 41500 国内在庫あり
JPY 100500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

現在のバッチを見る: 純度: 99.78%
99.78

Everolimus関連製品

シグナル伝達経路

mTOR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A549 Autophagy assay 5 uM 6 h Induction of autophagy in human A549 cells assessed as increase in conversion of LC3-1 to LC3-2 at 5 uM after 6 hrs by Western blot analysis 26176165
A549 Function Assay 5 uM 3 to 24 h Inhibition of mTOR phosphorylation at ser2448 in human A549 cells at 5 uM after 3 to 24 hrs by Western blot analysis 26176165
A549 Function Assay 5 uM 3 to 24 h Inhibition of mTOR in human A549 cells assessed as downregulation of p70S6K phosphorylation at thr389 at 5 uM after 3 to 24 hrs by Western blot analysis 26176165
OVCAR3 Cytotoxic Assay 72 h IC50=16 μM 24445311
DU145 Cytotoxic Assay 72 h IC50=8 μM 24445311
SK-HEP1 Cytotoxic Assay 72 h IC50=12 μM 24445311
CAKI1 Cytotoxic Assay 72 h IC50=14 μM 24445311
HT29 Cytotoxic Assay 72 h IC50=15 μM 24445311
HCT116 Cytotoxic Assay 72 h IC50=12 μM 24445311
ColoR Cytotoxic Assay 72 h IC50=8.7 μM 24445311
Colo205 Cytotoxic Assay 72 h IC50=20 μM 24445311
SQ20B Cytotoxic Assay 72 h IC50=5.5 μM 24445311
HOP62 Cytotoxic Assay 72 h IC50=19 μM 24445311
Colo205 Function Assay 24 h Inhibits mTORC1 in human COLO205 cells assessed as reduction of S6 phosphorylation at 0.1 to 8 uM 24836070
Colo205 Function Assay 24 h Inhibits mTORC1 in human COLO205 cells assessed as reduction of 4-EBP1 phosphorylation at 0.1 to 8 uM 24836070
SK-HEP1 Function Assay 24 h Inhibits mTORC1 in human SK-HEP1 cells assessed as reduction of S6 phosphorylation at 0.1 to 8 uM 24836070
SK-HEP1 Function Assay 24 h Inhibits mTORC1 in human SK-HEP1 cells assessed as reduction of 4-EBP1 phosphorylation at 0.1 to 8 uM 24836070
Sf9 Function Assay 15 to 20 mins Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay, IC50 = 2 μM. 23956101
Sf9 Function Assay 20 mins Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay, IC50 = 11.3 μM. 23956101
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生物活性

製品説明 エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。
Targets
FKBP12 [1]
(Cell-free assay)
mTOR (FKBP12) [1]
(Cell-free assay)
1.6-2.4 nM 1.6 nM-2.4 nM
In Vitro
In vitro 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]
Kinase Assay 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).
細胞実験 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot Mcl-1 / p-ERK / S6K1(T389) pS6RP cleaved caspase-3 27351224
Growth inhibition assay Cell counts IC50 Cell proliferation 27127803
Immunofluorescence TERT 27127803
In Vivo
In Vivo 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]
動物実験 動物モデル Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.
投与量 ≤2 mg/kg
投与経路 Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05843253 Not yet recruiting
High Grade Glioma|Diffuse Intrinsic Pontine Glioma|Anaplastic Astrocytoma|Glioblastoma|Glioblastoma Multiforme|Diffuse Midline Glioma H3 K27M-Mutant|Metastatic Brain Tumor|WHO Grade III Glioma|WHO Grade IV Glioma
Nationwide Children''s Hospital|Novartis
January 15 2024 Phase 2
NCT05501769 Recruiting
Breast Cancer
Arvinas Estrogen Receptor Inc.|Pfizer|Arvinas Inc.
September 8 2022 Phase 1
NCT05476939 Recruiting
Diffuse Intrinsic Pontine Glioma|Diffuse Midline Glioma H3 K27M-Mutant
Gustave Roussy Cancer Campus Grand Paris|Chimerix|Innovative Therapies For Children with Cancer Consortium
September 29 2022 Phase 3
NCT05293964 Recruiting
Breast Cancer
Jiangsu Simcere Pharmaceutical Co. Ltd.
May 18 2022 Phase 1

化学情報

分子量 958.22 化学式

C53H83NO14

CAS No. 159351-69-6 SDF Download Everolimus SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (104.36 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(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)

mg/kg g μL

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
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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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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