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化合物 AZD8055,AZD-8055

化合物 AZD8055|T1859|TargetMol

價(jià)格 172 378 622
包裝 1mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-02
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產(chǎn)品詳情

中文名稱:化合物 AZD8055英文名稱:AZD-8055
CAS:1009298-09-2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.
純度規(guī)格: 99.69%產(chǎn)品類別: 抑制劑
貨號: T1859
2024-12-02 化合物 AZD8055 AZD-8055 1mg/172RMB;5mg/378RMB;10mg/622RMB 172 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.69% 抑制劑

Product Introduction

Bioactivity

名稱AZD-8055
描述AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
細(xì)胞實(shí)驗(yàn)For growth inhibition and acridine staining, cells were exposed to increasing concentrations of AZD8055 for 72 to 96 h and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images were captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells were quantified. For LC3 assessment, cells were exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells were lysed on ice and analyzed by immunoblotting [1].
激酶實(shí)驗(yàn)The activity of mTOR was assayed using the recombinant mTOR technique described above. For inhibition experiments, AZD8055 was added to the reaction mixture and preincubated for 10 min before addition of ATP. Inhibition was performed at 1 to 3,000 nmol/L of AZD8055 in varying concentrations of ATP (40–200 μmol/L) [1].
動物實(shí)驗(yàn)Tumor cells (10^6 for U87-MG, 5 × 10^6 for A549) were injected s.c. in a volume of 0.1 mL, and mice were randomized into control and treatment groups when tumor size reached 0.2 cm^3. AZD8055 was formulated in 30% (w/v) captisol (pH 3.0). The control group received the vehicle only. Tumor volumes (measured by caliper), animal body weight, and tumor condition were recorded twice weekly for the duration of the study. The tumor volume was calculated (taking length to be the longest diameter across the tumor and width to be the corresponding perpendicular diameter) using the following formula: (length × width) × √(length × width) × (π/6) [1].
體外活性AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells [1]. In vitro, the median relative IC50 for AZD8055 against the PPTP cell lines was 24.7?nM. Relative I/O values >0% were observed in 8 cell lines and 15 cell lines showed Relative I/O values ranging from -4.7 to -92.2% [2].
體內(nèi)活性In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition [1]. AZD8055 administration could significantly decrease the IL-1β and TNF-α concentrations. Rats subjected to SAH + vehicle group demonstrated histological evidence of apoptosis compared with the sham group. The group treated with AZD8055 demonstrated a significant decrease in apoptosis ratio in the rat brain sample. In addition, in SAH group, the number of fluoro-jade B-positive cells clearly increased compared with the sham group. And the number of fluoro-jade B-positive cells decreased significantly in the SAH + rapamycin group and SAH + AZD8055 group [3].
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 3 mg/mL (6.44 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (96.66 mM)
關(guān)鍵字AZD8055 | inhibit | AZD-8055 | Apoptosis | mTOR | Mammalian target of Rapamycin | Inhibitor | Autophagy | AZD 8055
相關(guān)產(chǎn)品Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | 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 | 已知活性化合物庫 | 激酶抑制劑庫 | 高選擇性抑制劑庫 | 抗衰老化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫
關(guān)鍵字: AZD-8055|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(shí)體化合物分子供應(yīng);從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成;從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)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 (12年) 注冊資本 566.2651萬人民幣
員工人數(shù) 100-500人 年?duì)I業(yè)額 ¥ 1億以上
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)
  • TargetMol中國(陶術(shù)生物)
VIP 12年
  • 公司成立:12年
  • 注冊資本:566.2651萬人民幣
  • 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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