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曲美替尼,Trametinib

曲美替尼|T2125

價格 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: T2125
2024-12-02 曲美替尼 Trametinib 10mg/282RMB;25mg/452RMB;50mg/654RMB 282 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.88% 抑制劑

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)胞實驗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].
激酶實驗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].
動物實驗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 方法檢測細(xì)胞生長抑制情況。 結(jié)果:Trametinib 劑量依賴抑制 SB1、LD-1 和 EGI-1 細(xì)胞生長,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 方法檢測靶點蛋白表達(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,而不會發(fā)生早期凋亡。[3]
體內(nèi)活性方法:為檢測體內(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,表明在體內(nèi)具有抗腫瘤活性。[4] 方法:為檢測體內(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。[5]
存儲條件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 | 高選擇性抑制劑庫 | 抗衰老化合物庫 | 神經(jīng)退行性疾病化合物庫 | 酪氨酸激酶分子庫 | 藥物功能重定位化合物庫 | 疼痛相關(guān)化合物庫
關(guān)鍵字: 曲美替尼|||JTP-74057|||GSK1120212|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(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
  • 注冊資本:566.2651萬人民幣
  • 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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