Rapamycin (AY-22989)

Licensed by Pfizer 製品コード:S1039 別名:Rapamune, Sirolimus, NSC-2260804

For research use only.

Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

Rapamycin (AY-22989)化学構造

CAS No. 53123-88-9

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 52700
JPY 13600
JPY 46800
JPY 113200

代表番号: 03-5615-9297|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(1562)

製品安全説明書

mTOR阻害剤の選択性比較

相関mTOR製品

生物活性

製品説明 Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
ターゲット
mTOR [1]
(HEK293 cells)
~0.1 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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P31-FUJ NUfjNoNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfDXHN7UUN3ME2zNU42Ozd2IN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVMwLz6VQV7HSXI9N2F-
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U937 NFjSNYNCdnSrYnHjeIVzcWGuIFHzd4F6 M1nndFUxKM7:TR?= NWTIcYUzPDhiaB?= MmXCSG1UVw>? MUfJcoR2[2W|IHHueIlj[WO2ZYLpZYwh[WO2aY\peJkh[WejaX7zeEB4cWymIIT5dIUhVGWpaX;u[Yxt[SCybnX1cY9xcGmuYTDQbIlt[WSnbIDobYEuOSCMUkOyJIlvKFV7M{egZ4VtdHN? NGe5blA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG0NlExPid-MkGxOFIyODZ:L3G+
BT-20 MnrqT4lv[XOnIFHzd4F6 MlPBNlAh|ryP Mn;rSG1UVw>? MnvrSI9meyCwb4SgbY5pcWKrdDDtWG9TSzJiZHXw[Y5l\W62IIDBb3QhWzR5MzDwbI9{eGixconsZZRqd25? M3XTVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{WzOVUyLz5{MUO1N|U2OTxxYU6=
HEK293 MnvSSpVv[3Srb36gRZN{[Xl? MYKxNFAhdk1? MYq4JIg> MULEUXNQ MoPGTY5pcWKrdIOgWHBCNWmwZIXj[YQh\GWpcnHkZZRqd25ib3[gVIRk\DRid3n0bEBGSzVyIH;mJFUxKG6P MnPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3M{mzNFEoRjJzNUO5N|AyRC:jPh?=
PC3 Ml3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xMlUh|ryP MW[xJIg> NEfpWGFFVVOR NGPnS25KdmS3Y3XzJIFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kA9OTBibl2= MlL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7N{i2PFMoRjJzOUe4Olg{RC:jPh?=
PC3 NYroPHdwU2mwYYPlJGF{e2G7 NEGwelkyODBibl2= MWKxJIg> M3nTfmROW09? NF20ellFd2W|IH7veEBqdmirYnn0JI1VV1JvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?= M3frUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUe4Olg{Lz5{MUm3PFY5OzxxYU6=
PC3 M{PKbmtqdmG|ZTDBd5NigQ>? NGXHfJkyODBibl2= M2ji[FEhcA>? MnP6SG1UVw>? NU[yWYt6WG:2ZX70cJkhcW6qaXLpeJMhdVSRUj3t[YRq[XSnZDDTOkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDxzMDDuUU4> NEK4Ulg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm3PFY5Oyd-MkG5O|g3QDN:L3G+
HT-29 M2T6U2N6fG:2b4jpZ{BCe3OjeR?= MofoNVAhdk1? NVS1VlFHPzJiaB?= NIH4e4JFVVOR M4iwNHBwfGWwdHnheIV{KDVvZnz1c5JwfXKjY3nsMYlv\HWlZXSgZ5l1d3SxeHnjbZR6 M2jacFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFc{Lz5{NEmwNFg4OzxxYU6=
HT-29 NWDkXXpvS3m2b4TvfIlkKEG|c3H5 M1vBUFExKG6P NHO3eG44OiCq M2\RdmROW09? MVzQc5RmdnSrYYTld{BlcWerdH;4bY4ucW6mdXPl[EBkgXSxdH;4bYNqfHl? M1zBb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFc{Lz5{NEmwNFg4OzxxYU6=
HT-29 NYrvVG5jS3m2b4TvfIlkKEG|c3H5 MnTONVAhdk1? Mn\CO|IhcA>? NFu0[mpFVVOR NWrUU2tuWG:2ZX70bYF1\XNiY3HtdJRwfGinY3nuMYlv\HWlZXSgZ5l1d3SxeHnjbZR6 M{DpcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFc{Lz5{NEmwNFg4OzxxYU6=
HEK293 M1yyTWZ2dmO2aX;uJGF{e2G7 M4LKemlEPTBiPTCwMlAxODFizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN3MEm1N{c,OTd|NUC5OVM9N2F-
HEK293T, PBMCs NGfoW2RCdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= M3yzPVYh\GG7cx?= NWnqT4o{TUN3MDC9JFAvODByMTFOwG0> MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OEW1NFEoRjF5NEi1OVAyRC:jPh?=
HEK293T, PBMCs NYT0WZdRSW62aY\pdoFtKGGldHn2bZR6KGG|c3H5 MUS2JIRigXN? Mn;WSWM2OCB;IECuNFAyOyEQvF2= MlOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OEW1NFEoRjF5NEi1OVAyRC:jPh?=
cells from thymus of normal BALB/c mice MVTGeY5kfGmxbjDBd5NigQ>? MVXJR|UxKD1iMD6wNFMh|ryP M3\0S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyMEKxPVQ5Lz5zMECyNVk1QDxxYU6=
PC3 Mn3EcXRQWiCrbnjpZol1cW:wIHHzd4F6 M2nPS2lEPTBiPTCwMlAyKM7:TR?= NEHzPHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm3PFY5Oyd-MkG5O|g3QDN:L3G+
PC3 NFPib41CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M4H3eWlEPTBiPTCwMlAyKM7:TR?= NHfVRZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm3PFY5Oyd-MkG5O|g3QDN:L3G+
HEK293 NHXzZlFHfW6ldHnvckBCe3OjeR?= NEHiVVI5KGh? MXzFR|UxKD1iMD6wOUDPxE1? MlfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3M{mzNFEoRjJzNUO5N|AyRC:jPh?=
HeLa MoHiR5l1d3SxeHnjbZR6KGG|c3H5 NYHnW4lMUUN3MDC9JFAvPzdizszN MlPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMUWwO|AoRjNyMEG1NFcxRC:jPh?=
HEK293 Ml;3SpVv[3Srb36gRZN{[Xl? MoDsTWM2OCB;IEGuNUDPxE1? NY\VfFVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUS1N|A6ODdpPkG0OVMxQTB5PD;hQi=>
HCT-8 NEXkVmRHfW6ldHnvckBCe3OjeR?= M1\kW2lEPTBiPTCxMlI2KM7:TR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjJ|NUK2OUc,OTJ{M{WyOlU9N2F-
T47D MkfqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFnnNYk4OiCq MYDJR|UxKD1iMT61O|Yh|ryP M{nTd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{C4PFk2Lz5{OUOwPFg6PTxxYU6=
SiHa NFfBXJJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTaW204OiCq MYfJR|UxKD1iMT63OVYh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNyOEi5OUc,Ojl|MEi4PVU9N2F-
Lewis rat lymph node MoDPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NXvhfXJ6UUN3MDC9JFIvPiEQvF2= NYDITZl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[xPFU5PjVpPkG2NVg2QDZ3PD;hQi=>
MCF7 MnvpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlroO|IhcA>? M1jpWmlEPTBiPTC0Mlk5KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNyOEi5OUc,Ojl|MEi4PVU9N2F-
HepG2 (DPX-2) MmCxSpVv[3Srb36gRZN{[Xl? NYfLZpZbOjRiaB?= NHT1XZJGSzVyIE2gNVAh|ryP M4fqTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOU[2NFQ{Lz5{MEm2OlA1OzxxYU6=
Vero E6 MUjBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MUnJR|UxKD1iMk[uN|AzPyEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjN3M{i1PUc,OzJ|NUO4OVk9N2F-
PC3 NIrwNHBEgXSxdH;4bYNqfHliYYPzZZk> MWjFR|UxKD1iNEOuNUDPxE1? M3vGelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{e0OFI3Lz5{OEe3OFQzPjxxYU6=
アッセイ
Methods Test Index PMID
Western blot p-mTOR(S2448)/mTOR 23991038
Growth inhibition assay Cell proliferation 30393233
Histomorphology Haematoxylin & Eosin 28418837
Immunofluorescence NeuN ; p62/Beclin 28418837 28819214
ELISA Type III collagen/Fibronectin 23364979
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

  • 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

細胞試験:

[3]

  • 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.

動物試験:

[7]

  • 動物モデル:Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
  • 投薬量:~4 mg/kg/day
  • 投与方法:Injection i.p.

溶解度 (25°C)

体外

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):
2% DMSO+30% PEG 300+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

化学情報

分子量 914.18
化学式

C51H79NO13

CAS No. 53123-88-9
Storage 3年 -20°C
2年 -80°C in solvent
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

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。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05386914 Not yet recruiting Drug: Sirolimus Genetic Predisposition to Disease|Healthy Volunteers University of Missouri-Columbia July 2022 Phase 1
NCT04996719 Recruiting Drug: Rapamune Heart Failure Mayo Clinic May 24 2022 Phase 1
NCT05302791 Not yet recruiting Device: Muscle Cooling|Other: Resistance Exercise Exercise Training University of Nebraska May 2022 Not Applicable
NCT04989686 Withdrawn Other: Microsampling Immunosuppression Children''s Hospital of Philadelphia March 2022 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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。

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