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化合物 Tivantinib,Tivantinib

化合物 Tivantinib|T6117|TargetMol

價格 198 462 693
包裝 1mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-12
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產(chǎn)品詳情

中文名稱:化合物 Tivantinib英文名稱:Tivantinib
CAS:905854-02-6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: 99.41%產(chǎn)品類別: 抑制劑
貨號: T6117
2024-12-12 化合物 Tivantinib Tivantinib 1mg/198RMB;5mg/462RMB;10mg/693RMB 198 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.41% 抑制劑

Product Introduction

Bioactivity

名稱Tivantinib
描述Tivantinib (ARQ 197) is an orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity.
細(xì)胞實驗HT29, MKN-45, and MDA-MB-231 cells are seeded in black 96-well plates at 5 × 103 cells per well overnight in a medium with 10% FBS. The next day, cells are treated with increasing concentrations of ARQ-197 (0.03-10 μM) for 24, 32, and 48 hours at 37 °C. After ARQ-197 treatment, the drug-containing medium is removed and cells are incubated for at least 10 minutes in a labeling solution (10 mM HEPES, 140 mM NaCl, and 6 mM CaCl2) containing 2 μg/mL Hoescht 33342 (blue channel), 500-times diluted Annexin V-FITC (green channel), and 1 μg/mL propidium iodide (red channel). High-content image acquisition and analysis are carried out. The program is set to take four images per well. The exposure time is set at 16.7 ms/10% gain, 500 ms/35% gain, and 300 ms/30% gain for the 4,6-diamidino-2-phenylindole, FITC, and rhodamine channels, respectively. Images are processed and the numbers of positive cells for each channel and each condition are determined. In addition, HT29 cells are treated with increasing concentrations of ARQ-197 for 32 hours in the absence or the presence of 25, 50, and 100 μM ZvAD-FMK (irreversible general caspase inhibitor), and the same procedures are undertaken. All experiments are done in triplicate. To determine whether the apoptotic effect is due to c-Met inhibition, the effect of ARQ-197 when glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and c-Met are knocked down using siRNA is investigated. HT29, MKN-45, and MDA-MB-231 cells are transfected with a nontargeted control siRNA, a gapgh-targeted control siRNA, or a met-targeted siRNA. After 3 days, c-Met, GAPDH, and β-actin expression levels are determined using specific antibodies. To determine if the effect is caspase dependent, HT29, MKN-45, and MDA-MB-231 cells are transfected with a met-targeted siRNA for 2 days and incubated in the absence or the presence of increasing concentrations of ZvAD-FMK for 1 additional day.A nontargeted siRNA and a gapgh-targeted siRNA (siRNA GAPDH) are also transfected in parallel, as controls. Cells are then stained with Annexin V-FITC and propidium iodide, and the percentage of apoptotic cells is determined.(Only for Reference)
激酶實驗c-Met SDS-PAGE in vitro kinase assay: Recombinant c-Met protein (100 ng) is preincubated with increasing concentrations of ARQ-197 for 30 minutes at room temperature. Following preincubation, 100 μM of poly-Glu-Tyr substrate and various concentrations of ATP containing 5 μCi of [γ-32P]ATP are added to the reaction mixture. The reaction is incubated for 5 minutes at room temperature and then stopped by the addition of 5 μL of SDS-polyacrylamide gel, reducing sample buffer. The samples are then loaded onto a 7.5% acrylamide gel and SDS-PAGE is performed. The phosphorylated poly-Glu-Tyr substrates are ultimately visualized by autoradiography. c-Met activity is quantified by densitometry.
體外活性用ARQ-197處理的所有三種異種移植物模型顯示腫瘤生長減少:HT29模型中66%,MKN-45模型中45%,MDA-MB-231模型中79%.口服給藥200 mg/kg ARQ-197處理HT29,MKN-45和MDA-MB-231三種移植瘤模型,沒有顯著的體重變化.藥效學(xué)方面,ARQ-197強(qiáng)效抑制人類結(jié)腸移植瘤HT29中c-Met的磷酸化,單獨口服200 mg/kg ARQ-19724小時后,c-Met自磷酸化強(qiáng)烈下降.總之,ARQ-197抑制ARQ-197抑制c-Met依賴性異種移植人類腫瘤的生長.
體內(nèi)活性ARQ-197具有抗腫瘤活性,抑制A549,DBTRG和NCI-H441細(xì)胞增殖,IC50分別為0.38,0.45,0.29 μM。用ARQ-197處理,導(dǎo)致MAPK信號級聯(lián)反應(yīng)的磷酸化減少及預(yù)防侵入和遷移。此外,在沒有內(nèi)源性c-Met表達(dá)的細(xì)胞系NCI-H661中c-Met的異位表達(dá)導(dǎo)致其獲得侵襲性表型,也被ARQ-197抑制。ARQ-197抑制人類重組c-Met,具有恒定的Ki值,為355 nM。ARQ-197抑制c-Met磷酸化,且阻斷下游c-Met信號通路。盡管增加濃度的ARQ-197不會顯著影響ATP的Km,但c-Met暴露于0.5 μMARQ-197會使c-Met的Vmax降低約3倍。ARQ-197降低Vmax而不影響ATP的Km值說明ARQ-197抑制c-Met是非ATP競爭抑制,也說明ARQ-197具有高度激酶選擇性。ARQ-197抑制組成型和配體介導(dǎo)的c-Met自磷酸化,并且進(jìn)而抑制c-Met活性,繼而導(dǎo)致抑制下游c-Met效應(yīng)物。在表達(dá)c-Met的人類癌細(xì)胞(包括HT29,MKN-45和MDA-MB-231細(xì)胞)中ARQ-197誘導(dǎo)胱天蛋白酶依賴性細(xì)胞凋亡增加。
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 : 68 mg/mL (184.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字c-Met/HGFR | Tivantinib | inhibit | Apoptosis | ARQ-197 | ARQ197 | Inhibitor
相關(guān)產(chǎn)品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相關(guān)庫抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 高選擇性抑制劑庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 酪氨酸激酶分子庫 | 抗癌臨床化合物庫 | 抗癌藥物庫
關(guān)鍵字: ARQ 197|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓,致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個國家和地區(qū),已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫,以及多種類型的生化試劑產(chǎn)品,包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等,此外,我們還建設(shè)有CADD(計算機(jī)輔助藥物設(shè)計)研究中心、藥理實驗室、藥化合成平臺三大技術(shù)中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結(jié)果。
成立日期 2013-04-18 (12年) 注冊資本 566.265100萬人民幣
員工人數(shù) 100-500人 年營業(yè)額 ¥ 1億以上
主營行業(yè) 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) 經(jīng)營模式 貿(mào)易,工廠,試劑,定制,服務(wù)
  • TargetMol中國(陶術(shù)生物)
VIP 3年
  • 公司成立:12年
  • 注冊資本:566.265100萬人民幣
  • 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、藥物篩選等
  • 公司地址:靜安區(qū)江場三路238號8樓
詢盤

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