戈伐替尼|T6517|TargetMol

價(jià)格	￥148	￥347	￥548
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:戈伐替尼	英文名稱:Golvatinib
CAS:928037-13-2	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: ≥95%	產(chǎn)品類別: 抑制劑
貨號(hào): T6517

Product Introduction

Bioactivity

名稱	Golvatinib
描述	Golvatinib (E-7050) is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.
細(xì)胞實(shí)驗(yàn)	Cells (1–3 × 103 cells/100 μL/well) are seeded on 96-well culture plates with various concentrations of E7050 and cultured for 3 days. Then, 10 μL of WST-8 reagent is added to each well, and absorbance is measured at 450 nm compared with a reference measurement at 660 nm using a MTP-500 microplate reader. HUVEC (2 × 103 cells/well) are cultured for 3 days in medium containing HGF (30 ng/mL), VEGF (20 ng/mL), or basic fibroblast growth factor (bFGF) (20 ng/mL) together with serially diluted E7050.(Only for Reference)
激酶實(shí)驗(yàn)	Western blot analysis: The phosphorylation status of c-Met and VEGFR-2 is detected by Western blot analysis. For c-Met, MKN45 cells are incubated with a serial dilution of E7050 in complete medium at 37 °C for 2 h. For VEGFR-2, HUVEC are starved with human endothelial serum free medium containing 0.5% FBS for 24 h. Subsequently HUVEC are incubated with a serial dilution of E7050 for 1 h and then incubated with 20 ng/mL of human VEGF for 5 min. Cells are lysed by lysis buffer (50 mM HEPES [pH 7.4], 150 mM NaCl, 10% glycerol, 1% Triton X-100, 1.5 mM MgCl2, 1 mM EDTA [pH 8.0], 100 mM NaF, 1 mM phenylmethylsulfonyl fluoride 1 mM sodium orthovanadate, 10 μg/mL aprotinin, 50 μg/mL leupeptin, and 1 μg/mL pepstatin A). The resected tumor samples are homogenized with lysis buffer containing 25 mM β-glycerophosphate and 0.5% (v/v) phosphatase inhibitor cocktail 2 at 4 °C. Cellular debris is removed by centrifugation at 17 860 g for 20 min at 4 °C. Aliquots of the supernatants containing 5-20 μg of protein are subjected to SDS-PAGE under reducing conditions. The proteins are then transferred onto PVDF membranes, blocked with TBS containing 0.05% Tween-20 and either 5% skim milk or 5% BSA. The membranes are probed with the following antibodies: anti-c-Met polyclonal antibody (C-28) and anti-VEGFR-2 polyclonal antibody (C-20); mouse anti-phosphotyrosine clone 4 g10; and anti-VEGFR-2 polyclonal antibody, anti-phospho-VEGFR-2 (Tyr996) polyclonal antibody, and anti-phospho-c-Met (Tyr1234/1235) polyclonal antibody. Detection is performed using a Super Signal enhanced chemiluminescence kit. Immunoreactive bands are visualized by chemiluminescence with an Image Master-VDS-CL detection system. The intensity of each band is measured by using an image analyzer.
體外活性	體外研究表明，Golvatinib 強(qiáng)效抑制 c-Met 和 VEGFR-2 的磷酸化作用。Golvatinib 同時(shí)也強(qiáng)效抑制了經(jīng) HGF 或 VEGF 刺激的 c-met 擴(kuò)增腫瘤細(xì)胞和內(nèi)皮細(xì)胞的生長。[1] Golvatinib 通過在體外阻斷 Met/Gab1/PI3K/Akt 途徑，克服了由外源和/或內(nèi)源 HGF 引發(fā)的，對(duì)所有可逆的、不可逆的及突變選擇性的 EGFR-TKIs 耐藥性 EGFR 突變型肺癌細(xì)胞系的抵抗。Golvatinib 還能阻止因持續(xù)暴露于 HGF 而誘導(dǎo)的 gefitinib 抵抗性 HCC827 細(xì)胞的出現(xiàn)。[2]
體內(nèi)活性	在體內(nèi)研究中，使用Golvatinib展示了對(duì)腫瘤中c-Met與VEGFR-2磷酸化的抑制，以及異種移植模型中腫瘤生長和腫瘤血管生成的顯著抑制。對(duì)含有c-met擴(kuò)增的某些腫瘤細(xì)胞系用高劑量Golvatinib（50-200 mg/kg）處理，可誘導(dǎo)腫瘤退縮和消失。在腹膜播散模型中，Golvatinib對(duì)腹膜腫瘤顯示出抗腫瘤效果，并顯著延長了受治療小鼠的壽命。[1] 另一項(xiàng)異種移植模型研究中，由HGF轉(zhuǎn)染的Ma-1（Ma-1/HGF）細(xì)胞產(chǎn)生的腫瘤比載體對(duì)照腫瘤更易于血管生成，并表現(xiàn)出對(duì)ZD1839的抗性。Golvatinib單獨(dú)應(yīng)用可抑制血管生成并延緩Ma-1/HGF腫瘤的生長。Golvatinib與ZD1839聯(lián)合使用可顯著抑制腫瘤生長。[3]
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	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : ＜1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	Golvatinib \| c-Met/HGFR \| VEGFR \| E 7050 \| Inhibitor \| Vascular endothelial growth factor receptor \| E7050 \| inhibit
相關(guān)產(chǎn)品	Ribociclib \| Axitinib \| Sorafenib tosylate \| Lenvatinib mesylate \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| L-Ascorbic acid 2-phosphate trisodium \| Regorafenib monohydrate
相關(guān)庫	抑制劑庫 \| 抗癌活性化合物庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 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：戈伐替尼|||E-7050|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(gè)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(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)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。

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公司成立：12年
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