化合物 Tozasertib|T2509

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價(jià)格	￥348	￥668	￥996
包裝	10mg	25mg	50mg

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 Tozasertib	英文名稱:Tozasertib
CAS:639089-54-6	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: 99.99%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T2509

Product Introduction

Bioactivity

名稱	Tozasertib
描述	Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases.
細(xì)胞實(shí)驗(yàn)	Logarithmically growing MCF-7 cells were incubated with either VX-680 or DMSO for 48 h. Single-cell suspensions were fixed in 70% ethanol for 15 min, incubated with RNase (1 mg/ml) at 37 °C for 30 min, labeled with 400 μl propidium iodide (50 μg/ml) for at least 15 min at room temperature. Cell-cycle profiles were determined by flow cytometric analysis [1].
激酶實(shí)驗(yàn)	Recombinant Aurora-1 (62-344), Aurora-2 (1-403) and Aurora-3 (1-309) were expressed as N-terminal, His6-tagged fusion proteins using a baculovirus expression system. The proteins were purified by affinity chromatography using Ni-NTA agarose, followed by size exclusion using a Superdex 200 26/60 column. Inhibition of kinase activity was assessed using a standard enzyme-coupled system or a radiometric, phosphocellulose-peptide capture assay as previously described [1].
動(dòng)物實(shí)驗(yàn)	For the HL-60 study, female athymic NCr-nu mice were inoculated subcutaneously with 10^7 HL-60(TB) leukemia cells into the right axillary area. Treatment was administered i.p. b.i.d. after tumors reached 150–200 mm^3. VX-680 was prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. Cisplatin, formulated in saline, was administered i.p. q.4.d. for a total of three injections, at a dose of 5.4 mg/kg. For the MIA PaCa-2 studies, female MF1 nude mice were inoculated with 10^7 MIA PaCa-2 cells into the dorsal flank. Treatment was administered i.p. b.i.d. after tumors reached 175 mm^3. VX-680 was prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. 5-fluorouracil, formulated in saline, was administered i.v. q.4.d. at a dose of 50 mg/kg. For the HCT116 study, female Hsd RH rnu/nu rats were inoculated with 10^7 HCT116 cells into the right flank. Treatment was administered once the tumors reached 700–950mm^3. VX-680 was administered continuously through an indwelling femoral catheter, followed by a saline infusion for 4 d before repeating the dose cycle. For all studies, tumor volume was determined by caliper measurements three times a week [1].
體外活性	Tozasertib (VX-680) 是三種Aurora激酶的強(qiáng)效抑制劑，其表觀抑制常數(shù)（Ki（app））分別為Aurora-A、Aurora-B和Aurora-C的0.6、18及4.6 nM。VX-680導(dǎo)致細(xì)胞聚集在4N DNA含量處，并強(qiáng)力抑制了多種腫瘤細(xì)胞類(lèi)型的增殖，IC50值在15至113 nM之間[1]。不同的甲狀腺癌細(xì)胞（ATC細(xì)胞）經(jīng)VX-680處理后，其增殖在時(shí)間和劑量上表現(xiàn)出依賴性抑制，IC50值在25至150 nM之間。VX-680顯著阻礙了不同細(xì)胞系在軟瓊脂中形成菌落的能力。通過(guò)對(duì)半胱天冬酶-3活性的分析表明，VX-680在不同細(xì)胞系中誘導(dǎo)了凋亡[2]。
體內(nèi)活性	在裸鼠體內(nèi)，用Tozasertib以每日兩次，每次75 mg/kg的劑量通過(guò)腹腔注射(b.i.d. i.p.)治療13天后，與對(duì)照組相比，平均腫瘤體積減少了98%。在十只動(dòng)物中有四只的最終腫瘤體積比治療前的初始體積還要小。腫瘤生長(zhǎng)的減少與劑量成正比，且在12.5 mg/kg b.i.d.劑量下顯著。Tozasertib具有良好的耐受性，僅在最高劑量下觀察到體重輕微下降（75 mg/kg b.i.d.時(shí)，體重下降5%）。Tozasertib還在胰腺和結(jié)腸異種移植模型中誘導(dǎo)腫瘤退縮。在一個(gè)確立的人類(lèi)胰腺(MIA PaCa-2)異種移植模型中，用Tozasertib以每日兩次，每次50 mg/kg通過(guò)腹腔注射(b.i.d i.p.)治療，使得十個(gè)腫瘤中有七個(gè)出現(xiàn)退縮，并且與治療前的初始腫瘤體積相比，平均腫瘤體積減少了22% [1]。
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 : 40 mg/mL (86.1 mM)
關(guān)鍵字	VX680 \| inhibit \| Aurora Kinase \| Inhibitor \| VX-680 \| MK0457 \| MK 0457 \| Autophagy \| Tozasertib
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相關(guān)庫(kù)	經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 抗癌上市藥物庫(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) \| 酪氨酸激酶分子庫(kù) \| FDA 上市激酶抑制劑庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： VX 680|||MK-0457|TargetMol

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(zhuān)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(xiāo)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(lèi)企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

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