Rapamycin (Sirolimus)

別名:Rapamune, AY-22989, NSC-2260804

ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。

Rapamycin (Sirolimus)化学構造

CAS No. 53123-88-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 40500 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: 99.30%
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Rapamycin (Sirolimus)と併用されることが多い化合物

IKE(Imidazole ketone erastin)


Rapamycin and Imidazole ketone erastin induce cell death in ALL cell lines, resulting in a longer survival time for xenograft mice with ALL.


Zhu T, et al. Front Cell Dev Biol. 2021 Nov 15;9:740884.

Olaparib (AZD2281)


Rapamycin and Olaparib combination synergistically inhibit cell proliferation in non-small cell lung cancer (NSCLC) cells and triple-negative breast cancer (TNBC) cells, A549/H157/HCC1937/H522.


Osoegawa A, et al. Oncotarget. 2017 Jul 28;8(50):87044-87053

Oxaliplatin


Rapamycin and Oxaliplatin combination enhances the antitumor efficacy in A2780cis cells.


Liu J, et al. J Chemother. 2015;27(6):358-64.

Trametinib (GSK1120212)


Rapamycin and Trametinib combination enhances the antitumor activity in pediatric patient-derived xenograft (PDX) models.


Li F, et al. Clin Cancer Res. 2022 Sep 1;28(17):3836-3849.

MG132


Rapamycin and MG132 combination synergize the apoptotic and autophagic effects of curcumol in nasopharyngeal carcinoma.


Wang J, et al. Phytother Res. 2021 Dec;35(12):7004-7017.

Rapamycin (Sirolimus)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
U937 Antibacterial Assay 50 μM 48 h Induces antibacterial activity against wild type Legionella pneumophila Philadelphia-1 JR32 in U937 cells 21142106
HEK293 cells Kinase Assay 50 nM 45 min Inhibits mTOR kinase activity with IC50 of 0.1 nM 17350953
MCF-7 Autophagy Assay 30 nM 4 h Induces autophagy 20028134
PC3 Kinase Assay 100 nM 1 h Potently inhibits mTOR-mediated S6 phosphorylation with IC50 of <10 nM. 21978683
HeLa Function Assay 100 nM 36 h Induces FRB K2095P, T2098L, W2101F mutant-ubiquitinC interaction 17563385
SYF Function Assay 100 nM 24 h Induces FRB-FKBP complex interaction 17563385
HEK293 Function Assay 100 nM 8 h Inhibits TPA-induced degradation of Pdcd4 with EC50 of 50 nM 21539301
Drosophila melanogaster S2 cells transfected with N-luc and C-luc Function Assay 100 nM 4 h Induces luciferase protein trans-splicing in Drosophila melanogaster S2 cells transfected with N-luc and C-luc 17128262
cells from the thymus of normal BALB/c mice Growth Inhibition Assay 10 nM 72 h Inhibits lymphoproliferation (LAF) with IC50 of 3 nM 10021948
HT-29 Cytotoxic Assay 10 nM 72 h Potentiates digitoxin-induced cytotoxicity 24900873
PC3 Growth Inhibition Assay 1.5 μM 1 h Induces antiproliferative activity against human PC3 cells with IC50 of <10 nM 21978683
U87MG Kinase Assay 1 μM 6 h Potently inhibits mTOR-mediated S6 phosphorylation 19848404
PBMC Function Assay 1 nM 14 d Reduces CCR5 density 17485501
HEK293T Antiviral Assay 1 nM 4 d Induces antiviral activity against HIV1 X4 with EC50 of 0.3 nM 17485501
COS7 cells expressing EGFP-HDQ74/rheb Autophagy Assay 0.2 μM 24 h Induces autophagy 18391949
COS7 cells expressing EGFP-LC3 Autophagy Assay 0.2 μM 24 h Induces autophagy 18391949
H4 Function Assay 0.2 μM 24 h Increases the ratio of light chain 3 subunit 2 to light chain 3 subunit 1 in human H4 cells 18024584
Lewis rat lymph node cells Growth Inhibition Assay 5 μM IC50=2.6 μM 16185865
Human mixed lymphocyte Growth Inhibition Assay 5 nM IC50=1.6 nM. 16185865
BT-20 Kinase Assay 20 μM Does not inhibit mTORC2 dependent pAkT S473 phosphorylation 21353551
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生物活性

製品説明 ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。
Targets
mTOR [1]
(HEK293 cells)
~0.1 nM
In Vitro
In vitro

Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. [1] In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. [2] Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR. [3]

Kinase Assay Immunoblotting for the mTOR kinase assay
HEK293 cells are plated at 2-2.5×105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr
細胞実験 細胞株 U87-MG, T98G, and U373-MG
濃度 Dissolved in DMSO, final concentrations ~25 μM
反応時間 72 hours
実験の流れ

Cells are exposed to various concentrations of Rapamycin for 72 hours. For the assessment of cell viability, cells are collected by trypsinization, stained with trypan blue, and the viable cells in each well are counted. For the determination of cell cycle, cells are trypsinized, fixed with 70% ethanol, and stained with propidium iodide using a flow cytometry reagent set. Samples are analyzed for DNA content using a FACScan flow cytometer and CellQuest software. For apoptosis detection, cells are stained with the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) technique using an ApopTag apoptosis detection kit. To detect the development of acidic vesicular organelles (AVO), cells are stained with acridine orange (1 μg/mL) for 15 minutes, and examined under a fluorescence microscope. To quantify the development of AVOs, cells are stained with acridine orange (1 μg/mL) for 15 minutes, removed from the plate with trypsin-EDTA, and analyzed using the FACScan flow cytometer and CellQuest software. To analyze the autophagic process, cells are incubated for 10 minutes with 0.05 mM monodansylcadaverine at 37 °C and are then observed under a fluorescence microscope.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-mTOR(S2448)/mTOR 23991038
Growth inhibition assay Cell proliferation 30393233
Histomorphology Haematoxylin & Eosin 28418837
Immunofluorescence NeuN p62/Beclin 28418837
ELISA Type III collagen/Fibronectin 23364979
In Vivo
In Vivo

Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. [4] Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. [5] Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. [6] Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability. [7]

動物実験 動物モデル Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
投与量 ~4 mg/kg/day
投与経路 Injection i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06091332 Not yet recruiting
Cavernous Malformations|Brain Stem Hemorrhage
Huashan Hospital
December 1 2023 Phase 2
NCT05997056 Recruiting
Neuroendocrine Tumors|NET|Pancreatic Neuroendocrine Tumor|Gastrointestinal Neuroendocrine Tumor|Pulmonary Neuroendocrine Tumor
Aadi Bioscience Inc.
December 30 2023 Phase 2
NCT06022068 Enrolling by invitation
Alzheimer Disease
Karolinska Institutet|Karolinska University Hospital
September 1 2023 Phase 1|Phase 2
NCT04989686 Recruiting
Immunosuppression
Children''s Hospital of Philadelphia|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
June 8 2023 --
NCT05773326 Recruiting
High Grade Glioma|Glioma|Glioma Malignant|Glioblastoma
Nader Sanai|Barrow Neurological Institute|Ivy Brain Tumor Center|St. Joseph''s Hospital and Medical Center Phoenix
May 15 2023 Early Phase 1

化学情報

分子量 914.18 化学式

C51H79NO13

CAS No. 53123-88-9 SDF Download Rapamycin (Sirolimus) 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)O)C)C)O)OC)C)C)C)OC
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (109.38 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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