化合物 Adavosertib|T2077|TargetMol

價格	￥233	￥329	￥535
包裝	1mg	2mg	5mg

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 Adavosertib	英文名稱:Adavosertib
CAS:955365-80-7	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: 99.58%	產(chǎn)品類別: 抑制劑
貨號: T2077

Product Introduction

Bioactivity

名稱	Adavosertib
描述	Adavosertib (MK-1775) is a selective inhibitor of the cell cycle regulatory protein Wee1 (IC50=5.2 nM). Adavosertib has antitumor activity that blocks the cell cycle and inhibits tumor cell proliferation.
細胞實驗	Tumor cells were cultured in 96-well plates and incubated with DNA-damaging agents for 24 h, then with MK-1775 and nocodazole for additional 8 h. For p-CDC2Y15 assay, cells were lysed and subjected in a colorimetric ELISA to determine the amounts of p-CDC2Y15 (1:100) and total CDC2 (1:200). For phospho-histone H3 (pHH3), cells were fixed with methanol, stained with anti-pHH3 specific antibody and bound antibody was stained with Alexa Fluor 488 goat anti-rabbit antibody. Images were acquired with an INCell Analyzer 1000 [1].
激酶實驗	Kinase reaction was conducted with 10 μmol/L ATP, 1.0 μCi of [γ-33P]ATP, and 2.5 μg of poly(Lys, Tyr) as a substrate at 30°C for 30 min. Radioactivity incorporated into the substrate was trapped on MultiScreen-PH plates and was counted on a liquid scintillation counter [1].
動物實驗	Subcutaneous xenograft tumors were formed by injection of the human cancer cell lines in the hind flank of immunodeficient nude rats (F344/NJcl-rnu). To facilitate tumor formation, cells were injected in medium containing Matrigel, a solubilized basement membrane preparation extracted from the Engelbreth-Holm-Swarm mouse sarcoma. Gemcitabine, carboplatin, and cisplatin were dissolved or diluted in saline and were dosed i.v. MK-1775 was prepared in a vehicle of 0.5% methylcellulose solution and was dosed p.o. 24 h after dosing DNA-damaging agents. For efficacy studies, tumor volumes were measured with a caliper every 3 d and body weights were determined each weekday. Statistical analysis was done using repeated-measure ANOVA followed by Dunnett's test for relative tumor volume. T/C (%) was calculated as (ΔT/ΔC) × 100 if ΔT > 0 or (ΔT/TI) × 100 if ΔT < 0. ΔT was the change in mean tumor volume to the initial tumor volume for the treatment group, and ΔC was the change in mean tumor volume to the initial tumor volume for the vehicle control group. Ti was the initial tumor volume of the treatment group [1].
體外活性	方法：人結(jié)直腸癌細胞 WiDr 和人肺癌細胞 H1299 用 gemcitabine (0-100 nM) 處理 24 h，隨后用 Adavosertib (30-300 nM) 處理 24 h，使用 WST-8 assay 檢測細胞活力。結(jié)果：在 WiDr 細胞中，單獨 gemcitabine 在細胞活力測定中的 IC50 值大于 100.0 nmol/L。Adavosertib 聯(lián)合治療顯著增強了 gemcitabine 的抗生長作用。與 30 和 100 nmol/L 的 Adavosertib 共同處理將 IC50 分別降低到 21.5 和 7.1 nmol/L。在另一種 p53 缺乏型癌細胞系 H1299 中觀察到 gemcitabine 的類似增強作用。[1] 方法：人肺癌細胞 H1299 和 A549 用 Adavosertib (200 nmol/L) 處理 1 h，隨后后 7.5 Gy 照射 4-24 h，使用 flow cytometry 檢測細胞周期。結(jié)果：在用 Adavosertib + 輻射處理的 H1299 細胞中，細胞繼續(xù)進行 G2/M，沒有實質(zhì)性積累。與單獨輻射相比，Adavosertib 基本上沒有改變照射的 A549 細胞在 G2/M 中的積累。[2]
體內(nèi)活性	方法：為測試體內(nèi)抗腫瘤活性，用 Adavosertib (60 mg/kg，灌胃給藥) 和 1 Gy 福照處理攜帶人肺癌腫瘤 Calu-6 的 Ncr Nu/Nu 小鼠，每天兩次，持續(xù)五天。結(jié)果：藥物/輻射組合顯著增強了腫瘤生長延遲。當腫瘤每天兩次以 1Gy 照射 5 天，并且在照射的同一天每天兩次給予 60mg/kg Adavosertib 時，觀察到最大的反應(yīng)。[2]
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 (99.88 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.4 mg/mL (14.78 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	Adavosertib \| AZD-1775 \| AZD 1775 \| Wee1 \| inhibit \| MK 1775 \| MK1775 \| Inhibitor
相關(guān)產(chǎn)品	WEE1-IN-3 \| RP-6306 \| PD173952 \| ZN-c3 \| PD 407824 \| PKMYT1-IN-3 \| ZNL 02-096 \| Debio-0123 \| PD0166285 \| GSK-1520489A
相關(guān)庫	抑制劑庫 \| 抗乳腺癌化合物庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 高選擇性抑制劑庫 \| 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： MK-1775|||AZD1775|||Adavosertib (MK-1775)|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)和生物學研究的科學家提供優(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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