化合物 Adavosertib|T2077

價(jià)格	￥2490.00	￥1580.00	￥3490.00	￥329.00	￥4990.00	￥859.00	￥535.00	￥233.00	￥638.00	￥6970.00
包裝	50瓶	25瓶	100瓶	2瓶	200瓶	10瓶	5瓶	1瓶	1瓶	500瓶

最小起訂量	1瓶
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(guó)	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(hào): 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(xì)胞實(shí)驗(yàn)	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(shí)驗(yàn)	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(dòng)物實(shí)驗(yàn)	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(xì)胞 WiDr 和人肺癌細(xì)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(cè)細(xì)胞活力。結(jié)果：在 WiDr 細(xì)胞中，單獨(dú) gemcitabine 在細(xì)胞活力測(cè)定中的 IC50 值大于 100.0 nmol/L。Adavosertib 聯(lián)合治療顯著增強(qiáng)了 gemcitabine 的抗生長(zhǎng)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(xì)胞系 H1299 中觀察到 gemcitabine 的類似增強(qiáng)作用。[1] 方法：人肺癌細(xì)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(cè)細(xì)胞周期。結(jié)果：在用 Adavosertib + 輻射處理的 H1299 細(xì)胞中，細(xì)胞繼續(xù)進(jìn)行 G2/M，沒(méi)有實(shí)質(zhì)性積累。與單獨(dú)輻射相比，Adavosertib 基本上沒(méi)有改變照射的 A549 細(xì)胞在 G2/M 中的積累。[2]
體內(nèi)活性	方法：為測(cè)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(qiáng)了腫瘤生長(zhǎng)延遲。當(dāng)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(shí)，觀察到最大的反應(yīng)。[2]
存儲(chǔ)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) 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 \| ZNL 02-096 \| Debio-0123 \| PD0166285 \| GSK-1520489A
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗乳腺癌化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 高選擇性抑制劑庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： AZD1775|||MK-1775|||Adavosertib (MK-1775)

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)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(duì)明確靶點(diǎn)的分子篩選到對(duì)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(guò)在中國(guó)市場(chǎng)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(guò)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(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：12年
注冊(cè)資本：566.2651萬(wàn)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(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，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(chǎng)三路28號(hào)4樓

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