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化合物 Dinaciclib,Dinaciclib

化合物 Dinaciclib|T1912

價格 498 797 1240
包裝 2mg 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 Dinaciclib英文名稱:Dinaciclib
CAS:779353-01-4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: 99.75%產(chǎn)品類別: 抑制劑
貨號: T1912
2024-12-02 化合物 Dinaciclib Dinaciclib 2mg/498RMB;5mg/797RMB;10mg/1240RMB 498 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.75% 抑制劑

Product Introduction

Bioactivity

名稱Dinaciclib
描述Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.
細(xì)胞實驗A2780 cells were plated into six-well tissue culture dishes and allowed to adhere. Cells were then exposed to differing concentrations of SCH 727965 or a DMSO control vehicle for 24 hours, followed by a brief (30 min) pulsed exposure to bromodeoxyuridine (BrdUrd). Cells were then harvested, immunostained using FITC-conjugated antibodies specific for BrdUrd, counter-stained with propidium iodide/RNase A solution, and analyzed using flow cytometry. Fluorescence-activated cell sorting analyses were done on a FACSCalibur instrument. FITC-positive BrdUrd staining and propidium iodide signal allowed assessment of ongoing DNA replication and the cell cycle stage. Percentages of the cell population in each cell cycle stage were plotted for each test article concentration [1].
激酶實驗Recombinant cyclin/CDK holoenzymes were purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes were typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mmol/L Tris-HCl (pH 8.0), 10 mmol/L MgCl2, 1 mmol/L DTT, and 0.1 mmol/L sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μmol/L substrate solution (a biotinylated peptide derived from histone H1) were mixed and combined with 10 μL of diluted SCH 727965. The reaction was started by the addition of 50 μL of 2 μmol/L ATP and 0.1 μCi of 33P-ATP. Kinase reactions were incubated for 1 hour at room temperature and were stopped by the addition of 0.1% Triton X-100, 1 mmol/L ATP, 5 mmol/L EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads were captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads were washed twice with 2 mol/L NaCl and twice with 2 mol/L NaCl containing 1% phosphoric acid. The signal was then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves were generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values were derived by nonlinear regression analysis [1].
動物實驗For tumor implantation, specific cell lines were grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4 × 10^7 to 5 × 10^7 cells per milliliter. Nude mice were injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) were measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L × W × H)/2. When the tumor volume reached ~100 mm^3, the animals were randomized to treatment groups (10 mice/group) and treated i.p. with either SCH 727965 or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights were measured during and after the treatment periods. Data were expressed as means ± SEM. Animals were euthanized according to the Institutional Animal Care and Use Committee guidelines [1].
體外活性方法:人胰腺癌細(xì)胞系 MIAPaCa-2 和 Pa20C 用 Dinaciclib (0.5-128 nM) 處理 72 h,使用 MTT Assay 檢測細(xì)胞活力。 結(jié)果:Dinaciclib 以劑量依賴的方式抑制 MIAPaCa-2 和 Pa20C 細(xì)胞的生長,GI50 分別約為 10 和 20 nM。[1] 方法:人骨肉瘤細(xì)胞系 SaOs-2 和 U2OS 用 Dinaciclib (5-62 nmol/L) 處理 4-24 h,使用 Western Blot 檢測靶點(diǎn)蛋白表達(dá)水平。 結(jié)果:Dinaciclib 消除骨肉瘤細(xì)胞中 CDK 底物的磷酸化。[2]
體內(nèi)活性方法:為檢測體內(nèi)抗腫瘤活性,將 Dinaciclib (40 mg/kg,20% (w/v) HPBCD) 腹腔注射給攜帶人胰腺癌腫瘤 JH033 或 Panc286 的 CD1 nu/nu athymic 小鼠,每周兩次,持續(xù)四周。 結(jié)果:Dinaciclib 抑制一組低滲透癌癥異種移植物的體內(nèi)生長。[1] 方法:為檢測體內(nèi)抗腫瘤活性,將 Dinaciclib (8-48 mg/kg) 腹腔注射給攜帶卵巢癌腫瘤 A2780 的 BALB/c 小鼠,每天一次,持續(xù)十天。 結(jié)果:Dinaciclib 在體內(nèi)具有劑量依賴性的抗腫瘤活性,并且在低于 MTD 的劑量水平下幾乎完全抑制腫瘤生長。[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DMSO : 50 mg/mL (126.11 mM)
Ethanol : 8 mg/mL (20.17 mM), Heating is recommended.
關(guān)鍵字inhibit | Inhibitor | SCH727965 | Cyclin dependent kinase | CDK | Apoptosis | PS095760 | PS 095760 | Dinaciclib | SCH-727965
相關(guān)產(chǎn)品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相關(guān)庫抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌上市藥物庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | FDA 上市激酶抑制劑庫 | 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: SCH 727965|||PS-095760|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(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 年營業(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
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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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