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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | RAD001,SDZ-RAD | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C53H83NO14 |
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| 分子量 | 958.22 | CAS No. | 159351-69-6 | |
| Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (104.36 mM) | |
| Ethanol | 100 mg/mL (104.36 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
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) と 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。 |
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| in vitro | Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. This compound 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] It 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 this chemical 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 this compound and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %. [3] |
| 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, this compound 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 this compound and trastuzumab significantly decreases the xenograft tumor size (410.8 mm3) more than this compound treatment alone. [3] |
プロトコル(参考用のみ)
| キナーゼアッセイ | FKBP12 binding assay & Mixed lymphocyte reaction (MLR) | |
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| 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 of this compound/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 of this compound/IC50 RAP). | ||
| 細胞アッセイ | 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 this compound 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 this compound 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 this chemical (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 this compound. | |
| 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. |
| 投薬量 | ≤2 mg/kg | |
| 投与方法 | Administered via p.o. | |
参考
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カスタマーフィードバック
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Data from [Data independently produced by Br J Cancer, 2014, 111(6), 1168-79]
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Data from [Data independently produced by Clin Cancer Res, 2013, 19(3),598-609]
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Data from [Data independently produced by Cancer Cell, 2012, 21(2), 155-67]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14] | PubMed: 40185092 |
| Ataluren improves hematopoietic and pancreatic disorders in Shwachman-Diamond syndrome patients: a compassionate program case-series [ Nat Commun, 2025, 16(1):8189] | PubMed: 40897730 |
| Haploinsufficiency of miR-143 and miR-145 reveal targetable dependencies in resistant del(5q) myelodysplastic neoplasm [ Leukemia, 2025, 39(4):917-928] | PubMed: 40000845 |
| Pancreatic Neuroendocrine Tumors Secrete Apolipoprotein E to Induce Tip Endothelial Cells That Remodel the Tumor-Stroma Ratio and Promote Cancer Progression [ Cancer Res, 2025, 85(15):2805-2819] | PubMed: 40623046 |
| Targeting the MYC oncogene with a selective bi-steric mTORC1 inhibitor elicits tumor regression in MYC-driven cancers [ Cell Chem Biol, 2025, 32(8):994-1012.e11] | PubMed: 40803322 |
| YAP1 promoter-associated noncoding RNA affects Ewing sarcoma cell tumorigenicity by regulating YAP1 expression [ Cell Mol Biol Lett, 2025, 30(1):63] | PubMed: 40414844 |
| Increased fatty acid delivery by tumor endothelium promotes metastatic outgrowth [ JCI Insight, 2025, 10(9)e187531] | PubMed: 40198126 |
| Molecular control of PDPNhi macrophage subset induction by ADAP as a host defense in sepsis [ JCI Insight, 2025, e186456] | PubMed: 39903516 |
| A phase II trial of mTORC1/2 inhibition in STK11 deficient non small cell lung cancer [ NPJ Precis Oncol, 2025, 9(1):67] | PubMed: 40069402 |
| Enhancing immunotherapy through PD-L1 upregulation: the promising combination of anti-PD-L1 plus mTOR inhibitors [ Mol Oncol, 2025, 19(1):151-172] | PubMed: 39258533 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。