曲美替尼|T2125

價(jià)格	￥282	￥452	￥654
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:曲美替尼	英文名稱:Trametinib
CAS:871700-17-3	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: 99.88%	產(chǎn)品類別: 抑制劑
貨號(hào): T2125

Product Introduction

Bioactivity

名稱	Trametinib
描述	Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
細(xì)胞實(shí)驗(yàn)	These cells were maintained in media recommended by the providers. Exponentially growing cells were precultured in 96-well tissue culture plates for 24 h and then exposed to JTP-74057. Cell growth was determined by an in vitro toxicology assay kit, sulforhodamine B based. For combination studies, two compounds were simultaneously added to the HT-29 cells and incubated for 72 h. In the presence of various concentrations of compound A, the 50% inhibitory concentration (IC50) values of compound B were determined. Then, the fixed concentration of compound A versus the IC50 value of compound B was plotted. Conversely, the IC50 values of compound A were determined in the presence of various concentrations of compound B and plotted [1].
激酶實(shí)驗(yàn)	A Raf-MEK-ERK cascade kinase assay was carried out as previously described. Briefly, nonphosphorylated myelin basic protein (MBP) was coated onto an ELISA plate, and the active form of B-Raf/c-Raf was mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of JTP-74057. The phosphorylation of MBP was detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases were tested by kinase profiler at 10 μM ATP [1].
動(dòng)物實(shí)驗(yàn)	Female BALB/c-nu/nu mice were used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) were inoculated subcutaneously into the right flank of the mice at 5x10^6 cells/100 μl/site or 1x10^6 cells/100 μl/site, respectively. The acetic acid-solvated form of JTP-74057 was dissolved in 10% Cremophor EL-10% PEG400 and was administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm^3. The tumor length [L (mm)] and width [W (mm)] were measured using a micro gauge twice a week after the commencement of dosing, and the tumor volume was calculated using the following formula: tumor volume (mm^3) = L x W x W/2. All procedures relating to the use of animals in this study were reviewed and approved by the Institutional Animal Care and Use Committee of Japan Tobacco [1].
體外活性	方法：小鼠肝內(nèi)膽管癌細(xì)胞 SB1、LD-1 和人肝內(nèi)膽管癌細(xì)胞 EGI-1 用 Trametinib (0-10000 nM) 處理 48 h，使用 MTT 方法檢測(cè)細(xì)胞生長(zhǎng)抑制情況。結(jié)果：Trametinib 劑量依賴抑制 SB1、LD-1 和 EGI-1 細(xì)胞生長(zhǎng)，IC50 分別為 41.48 nM、56.10 nM 和 27.89 nM。[1] 方法：人結(jié)腸癌細(xì)胞 RKO 用 Trametinib (200 nmol/L) 處理 30 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Trametinib 顯著降低 p-ERK 和 p-AKT 水平。[2] 方法：人膠質(zhì)瘤細(xì)胞 U87 和 U251 用 Trametinib (50 nM) 孵育 6-72 h，使用 Flow Cytometry 方法檢測(cè)細(xì)胞凋亡情況。結(jié)果：Trametinib 誘導(dǎo) U87 和 U251 細(xì)胞的凋亡率明顯增加。Trametinib 可以誘導(dǎo)神經(jīng)膠質(zhì)瘤細(xì)胞的晚期凋亡，而不會(huì)發(fā)生早期凋亡。[3]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Trametinib (0.3-1 mg/kg) 口服給藥給攜帶人結(jié)直腸癌腫瘤 HT-29 和 COLO205 的 BALB/c-nu/nu 小鼠，每天一次，持續(xù)十四天。結(jié)果：Trametinib 治療顯著抑制人結(jié)直腸癌腫瘤的生長(zhǎng)，表明在體內(nèi)具有抗腫瘤活性。[4] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Trametinib (5 mg/kg) 腹腔注射給攜帶人B淋巴細(xì)胞白血病腫瘤 KOPN8 和 COLO205 的 NSG 小鼠，每周三次，持續(xù)十四天。結(jié)果：Trametinib 單藥治療延緩了白血病的進(jìn)展，但不足以防止白血病的生長(zhǎng)。[5]
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	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.1 mg/mL (3.41 mM), Suspension. 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. DMSO : 7.86 mg/mL (12.77 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	inhibit \| MAP2K \| Apoptosis \| Autophagy \| Inhibitor \| Trametinib \| orally \| type \| MAPKK \| collageninduced \| MEK \| arthritis \| AIA \| GSK 1120212 \| JTP74057 \| Mitogen-activated protein kinase kinase \| GSK-1120212 \| Adjuvant-induced \| JTP 74057 \| CIA
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(kù)	經(jīng)典已知活性庫(kù) \| 抗癌上市藥物庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 高選擇性抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| 神經(jīng)退行性疾病化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 藥物功能重定位化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù)

關(guān)鍵字：曲美替尼|||JTP-74057|||GSK1120212|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)

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公司成立：12年
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