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依維莫司,Everolimus
  • 依維莫司,Everolimus

依維莫司|T1784|TargetMol

2篇文獻
價格 196 435 655
包裝 1mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2025-03-12
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產(chǎn)品詳情

中文名稱:依維莫司英文名稱:Everolimus
CAS:159351-69-6品牌: TargetMol
產(chǎn)地: 美國保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.78%產(chǎn)品類別: 抑制劑
貨號: T1784
2025-03-12 依維莫司 Everolimus 1mg/196RMB;5mg/435RMB;10mg/655RMB 196 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. 99.78% 抑制劑

Product Introduction

Bioactivity

名稱Everolimus
描述Everolimus (SDZ-RAD) is a derivative of Rapamycin, an mTOR1 inhibitor with selective and oral activity. Everolimus exhibits immunosuppressive and antitumor activity, inhibiting tumor cell proliferation, inducing apoptosis and autophagy.
細胞實驗BT474 stem cells that were sorted by flow cytometry were cultured in stem cell culture medium in 25-ml cell culture flasks. The cells were divided into four groups: (1) the control group (blank control), (2) the Ever group (100 nM everolimus), (3) the Tz group (10 μg/ml trastuzumab), and (4) the Ever+Tz group (100 nM everolimus and 10 μg/ml trastuzumab). Culture medium with 0.5 % DMSO was added to the blank control group. After treatment, the cells were cultured in an incubator at 37 °C with 5 % CO2 for 24 h before the cells were collected. For cell cycle determination, the cells in the different treatment groups were fixed in ice-cold ethanol for 24 h. The ethanol was removed, 500 μl RNase-containing propidium iodide (PI) and 1 mL PBS were added, and the cells were incubated at 4 °C for 30–60 min in the dark. The samples were then sorted by flow cytometry according to each cell cycle stage, and G0/G1 %, S%, and G2/M% were calculated to obtain the cell cycle distribution. To understand the effect of drug treatment on stem cell apoptosis, annexin-FITC and PI were added to the single-cell suspension and mixed well before incubation at room temperature for 5–15 min in the dark. The cells were then sorted by flow cytometry within 1 h after incubation to measure the rate of apoptosis [3].
激酶實驗Binding to the FK 506 binding protein (FKBP12) was indirectly assessed by means of an ELISA-type competition assay. FK 506 was included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to FK 506 (rIC50 5 IC50 test compound/IC50 FK 506). Details regarding this assay have been reported [1].
動物實驗Cultured BT474 stem cells were collected and pelleted by centrifugation at 1,000 rpm for 5 min. The cells were then washed with serum- and antibiotics-free DMEM medium three times. After the cells were counted, aliquots of cells at 1×10^5/100 μl in serum- and antibiotic-free culture medium in (microcentrifuge tubes) were sent to the animal room under sterile conditions. A volume of 100 μl stem cell suspension was injected beneath the left breast pad of BALB/c nude mice. The injected mice were housed in clean cages under a constant temperature of 20–25 °C with free access to food and water. When the tumor volume was approximately 300 mm3 (approximately 9 days after stem cell injection), the tumor-bearing mice were randomly divided into four groups (five animals/group): (1) the control group (normal saline), (2) the Ever group (2 mg/kg everolimus), (3) the Tz group (5 mg/kg trastuzumab), and (4) the Ever+Tz group (2 mg/kg everolimus and 5 mg/kg trastuzumab); this day was denoted as day 1. Thereafter, the greatest longitudinal diameter (L) and the greatest transverse diameter (W) of the xenograft tumors in mice were measured by caliper in the morning once every 3 days, and tumor volumes were calculated and recorded when the test articles were administered. After the last tumor volume measurement on day 16, the mice were euthanized by cervical dislocation, and tumor specimens were collected and fixed for histochemical assays [3].
體外活性方法:原發(fā)性乳腺癌細胞和 BT474 細胞用 Everolimus (0.001-10 μM) 處理 24 h,使用 MTT assay 檢測細胞活力。 結(jié)果:Everolimus 對原發(fā)性乳腺癌細胞和 BT474 細胞具有劑量依賴性抑制作用,IC 50 分別為 156 nM 和 71 nM。[1] 方法:乳腺癌細胞 MCF-7 和 BT474 用 Everolimus (5 mg/mL) 處理 48 h,使用 Flow cytometry 檢測細胞凋亡情況。 結(jié)果:Everolimus 在孵育 48 h 后誘導(dǎo) MCF-7 和 BT474 細胞的凋亡。[2]
體內(nèi)活性方法:為測試體內(nèi)抗腫瘤活性,將 Everolimus (5-10 mg/kg in 0.5% CMC) 灌胃給藥給攜帶乳腺癌腫瘤 MC4-L2 的 BALB/c 小鼠,每周五次,持續(xù)二十天。 結(jié)果:10 mg/kg 和 5 mg/kg 劑量的 Everolimus 都能有效抑制腫瘤生長,從而減少乳腺腫瘤體積。[3]
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (5.22 mM), Solution.
Ethanol : 50 mg/mL (52.18 mM), Sonication is recommended.
DMSO : 50 mg/mL (52.18 mM), Sonication is recommended.
H2O : Insoluble
關(guān)鍵字RAD-001 | RAD 001 | mTOR (FKBP12) | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit | FKBP | FK506-binding protein | Everolimus | Autophagy | Apoptosis
相關(guān)產(chǎn)品Naringin | Guanidine hydrochloride | L-Glutamic acid | Gefitinib | Cysteamine hydrochloride | Alginic acid | Hydroxychloroquine | Stavudine | Dextran sulfate sodium salt (MW 4500-5500) | L-Ascorbic acid sodium salt | Paeonol | Sodium 4-phenylbutyrate
相關(guān)庫抑制劑庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 臨床失敗化合物庫 | EMA 上市藥物庫 | FDA 上市藥物庫 | 免疫/炎癥分子化合物庫 | FDA 上市激酶抑制劑庫 | 抗癌臨床化合物庫
關(guān)鍵字: 依維莫司|||SDZ-RAD|||RAD001|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部,化學(xué)事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實體化合物分子供應(yīng);從商業(yè)化產(chǎn)品銷售到個性化定制合成;從對明確靶點的分子篩選到對明確分子的多靶點篩選,從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化,我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。 經(jīng)過在中國市場五年的精心耕耘,我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商,為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期 2013-04-18 (13年) 注冊資本 566.2651萬人民幣
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主營行業(yè) 化學(xué)試劑,生物活性小分子 經(jīng)營模式 貿(mào)易,試劑,定制,服務(wù)
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VIP 13年
  • 公司成立:13年
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  • 企業(yè)類型:有限責(zé)任公司(自然人投資或控股)
  • 主營產(chǎn)品:小分子抑制劑,藥物篩選化合物庫,天然產(chǎn)物,活性分子化合物等
  • 公司地址:上海市閘北區(qū)江場三路28號4樓
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