Rapamycin

別名：AY-22989, NSC-2260804

製品コード：S1039 純度：99.63%

ラパマイシン (Rapamycin (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。

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
5mg	JPY 22000	国内在庫あり
25mg	JPY 40500	国内在庫あり
100mg	JPY 100500	国内在庫あり
1g	JPY 220500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（1743）

製品安全説明書

現在のバッチを見る：純度： 99.63%

99.63

Rapamycin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.

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.

Y-27632 2HCl

Explore the effect of both on epigenetic ageing.

Horvath S, et al. Aging (Albany NY). 2019;11(10):3238-3249.

Z-VAD-FMK

Combined use reduces photoreceptor necrosis and preserve the ONL thickness after retinal detachment.

Ding J, et al. Curr Eye Res. 2019;44(7):739-745.

SB431542

Explore role of TGFβ receptor in rapamycin-induced upregulation of CTGF Expression.

Wu Y, et al. Front Pharmacol. 2018 Aug 8;9:877.

Rapamycin関連製品

関連ターゲット	mTORC1 mTORC2	もっと見る
関連製品	AZD8055 Torin 1 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128) Torkinib (PP242) Vistusertib (AZD2014) MHY1485 KU-0063794 Torin 2 OSI-027 WYE-354 WYE-125132 (WYE-132) 3BDO Palomid 529 (P529) Zotarolimus (ABT-578) Salidroside GDC-0349 WAY-600 Onatasertib (CC 223) XL388 WYE-687	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

mTOR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 (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
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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06308445	Not yet recruiting	Familial Adenomatous Polyposis	University Hospital Toulouse	August 1 2024	Phase 2
NCT06310291	Not yet recruiting	Celiac Disease	Barinthus Biotherapeutics	April 2024	Early Phase 1
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.	November 7 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	--

参考
[1] Edwards SR, et al. J Biol Chem, 2007, 282(18), 13395-13401. [2] Barbet NC, et al. Mol Biol Cell, 1996, 7(1), 25-42. [3] Takeuchi H, et al. Cancer Res, 2005, 65(8), 3336-3346. [4] Bodine SC, et al. Nat Cell Biol, 2001, 3(11), 1014-1019. [5] Kenerson HL, et al. Cancer Res, 2002, 62(20), 5645-5650. [6] Guba M, et al. Nat Med, 2002, 8(2), 128-135. [7] Phung TL, et al. Cancer Cell, 2006, 10(2), 159-170. [8] MG Mohi, et al. Proc Natl Acad Sci U S A, 2004, 101(9), 3130–3135. [9] Rangaraju S, et al. J Neurosci. 2010 Aug 25;30(34):11388-97. + 展開

参考

+ 展開

化学情報

分子量	914.18	化学式	C₅₁H₇₉NO₁₃
CAS No.	53123-88-9	SDF	Download Rapamycin 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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

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 : 25 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
	Clear solution	1%DMSO 1 40%PEG300 2 5%TWEEN80 3 54%ddH2O	0.6mg/ml (0.66mM)	Taking the 1 mL working solution as an example, add 10 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 540 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 Corn oil	5.0mg/ml (5.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	1% DMSO 1 40% PEG 300 2 5%Tween80 3 54% water	0.25mg/ml (0.27mM)	Taking the 1 mL working solution as an example, add 10 μL of 25 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue adding 540 μL ddH2O and adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil	5.0mg/ml (5.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml (5.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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